.

Синтез, фізико-хімічні та біологічні властивості 3-заміщених 4-гідрокси-2-оксохінолінів: Автореф. дис… канд. фармац. наук / О.А. Євтіфєєва, Укр. фар

Язык: украинский
Формат: реферат
Тип документа: Word Doc
0 1267
Скачать документ

22

OE?A?INUeEA OA?IAOeAAOE*IA AEAAeAI?ss

wmetafile8? ?????Z????????&??yyyy????MrEd?Microsoft
Draw??Z???&?©?MrEd?????

?AO?O??AA Ieueaa Aiaoie??aia

OAeE 547.831.7/8:54.04:54.057

NEIOAC, O?CEEI-O?I?*I? OA A?IEIA?*I? AEANOEAINO? 3-CAI?UAIEO
4-A?Ae?IENE-2-IENI-O?IIE?I?A

15.00.02 – oa?iaoeaaoe/ia o?i?y ? oa?iaeiaiic?y

AAOI?AOA?AO

aeena?oaoe?? ia caeiaoooy iaoeiaiai nooiaiy

eaiaeeaeaoa oa?iaoeaaoe/ieo iaoe

Oa?e?a – 1999

Aeena?oaoe??th ? ?oeiien.

?iaioa aeeiiaia ia eaoaae?? oa?iaoeaaoe/ii? o?i?? Oe?a?inueei?
oa?iaoeaaoe/ii? aeaaeai??, I?i?noa?noai ioi?iie caei?ia’y Oe?a?ie.

Iaoeiaee ea??aiee: eaiaeeaeao oa?iaoeaaoe/ieo iaoe, aeioeaio

OA?AI Na?oeaia A?eai??aia

Oe?a?inueea oa?iaoeaaoe/ia aeaaeai?y, aeioeaio

eaoaae?e oa?iaoeaaoe/ii? o?i??

Io?oe?ei? iiiiaioe: aeieoi? o?i?/ieo iaoe, i?ioani?

AIEIOIA Aaea??e Aaneeueiae/

Oe?a?inueea oa?iaoeaaoe/ia aeaaeai?y, caa?aeoth/ee

eaoaae?ith aiae?oe/ii? o?i??

aeieoi? oa?iaoeaaoe/ieo iaoe, i?ioani?

IAOTHI?I Aaiaae?e Iaaeiae/

Oa?e?anueeee ?inoeooo oaeineiiaeaiiy e?ea??a,

caa?aeoth/ee eaoaae?ith ee?i?/ii? a?io?i?? ? noaeiai-

iaaee/ii? oieneeieia??

I?ia?aeia onoaiiaa: Aea?aeaaiee iaoeiaee oeaio? e?ea?nueeeo cania?a

(i. Oa?e?a), eaai?aoi??y aeiiii?aeieo o?i?ei-

oa?iaoeaaoe/ieo ?a/iaei oa e?iainieiieo

iaoa??ae?a

Caoeno a?aeaoaeaoueny “ 16 ” ea?oiy 1999 ?ieo i __1200__ aiae.
ia can?aeaii? niaoe?ae?ciaaii? a/aii? ?aaee Ae 64.605.01 i?e
Oe?a?inuee?e oa?iaoeaaoe/i?e aeaaeai?? ca aae?anith: 310002, i. Oa?e?a,
aoe. Iooe?inueea, 53.

C aeena?oaoe??th iiaeia iciaeiieoeny a a?ae?ioaoe? Oe?a?inueei?
oa?iaoeaaoe/ii? aeaaeai?? (310168, i. Oa?e?a, aoe. Aethoa?a, 4).

Aaoi?aoa?ao ?ic?neaiee “__13__”___aa?aciy_____ 1999 ?.

A/aiee nae?aoa? A?EOeAIEI ?.N.

niaoe?ae?ciaaii? a/aii? ?aaee

CAAAEUeIA OA?AEOA?ENOEEA ?IAIOE

Aeooaeuei?noue oaie. ?icoe?aiiy a?naiaeo no/anieo e?ea?nueeeo cania?a
oeyoii noai?aiiy iiaeo aoaeoeaieo ? iaeioiene/ieo i?ea?iaeueieo
e?ea?nueeeo i?aia?ao?a — iaeia c iaeaaaeeea?oeo caaea/ oa?iaoeaaoe/ii?
iaoee oa i?aeoeee. Iaeiei c aoai?a ae??oaiiy oe??? i?iaeaie ?
oe?eani?yiiaaiee iiooe a?ieia?/ii aeoeaieo noanoaioe?e, aea/aiiy ?o
oa?iaeieia?/ieo oa o?ceei-o?i?/ieo oa?aeoa?enoee, anoaiiaeaiiy ca’yceo
i?ae no?oeoo?ith niieoe oa ?o oa?iaeieia?/iith ae??th.

Oe?iea canoinoaaiiy a iaaee/i?e i?aeoeoe? ciaeoee iio?aei? o?iie?io:
aioei?e?iai? caniae — ooi?o?iieiie (ii?oeienaoeei, iaoeienaoeei,
eiiaoeienaoeei oa ?io.), i?o?ienie?i; aiaeueaaoee — aeaoai?i;
a?iioie?oee — ooaeaiao?i; i?ioeiaey??ei? i?aia?aoe — o?iioeeae ?
ieaeaai?e oa aaaaoi ?ioeo.

Iia? iioaioe?ei? iiaeeeaino? a oeueiio ieai? iathoue 3-cai?uai?
4-a?ae?iene-2-ienio?iie?ie. Ia eaoaae?? oa?iaoeaaoe/ii? o?i??
Oe?a?inueei? oa?iaoeaaoe/ii? aeaaeai?? neioaciaaii iio?aeia
4-a?ae?iene-2-ienio?iie?io — aoaeoeaiee i?aia?ao i?noeaaiaianoacoth/i?
ae??, yeee c oni?oii i?ioiaeeoue ee?i?/i? aei?iaoaaiiy; iaea?aeaii
?a/iaeie c ae?aaeaiith aioeoe?ai?aeiith, i?ioei?e?iaiith,
i?ioecaiaeueiith aeoeai?noth. C ae?oaiai aieo ?ioa?an aei oeeo niieoe
iiynith?oueny oei, ui na?aae i?e?iaeieo a?ieia?/ii aeoeaieo ?a/iaei
o?iie?iiai? no?oeoo?e naia 3-cai?uai? a?ae?iene(ieni)o?iie?io (a oiio
/ene? — 3-aee?ecai?uai?) i?aaenoaaeai? iaea?eueo oe?iei, oa ?acii c oei,
i?aeoe/ii ia aea/aia ?o a?ieia?/ia aeoeai?noue.

Ca’ycie ?iaioe c iaoeiaeie i?ia?aiaie, ieaiaie, oaiaie. Aeena?oaoe?y
aeeiiaia ca?aeii c ieaiii iaoeiai-aeine?aeieo ?ia?o Oe?a?inueei?
oa?iaoeaaoe/ii? aeaaeai?? c i?iaeaie IIC Oe?a?ie (iiia? aea?aeaaii?
?a?no?aoe?? 01.91.0002385).

Iaoa ? caaea/? aeine?aeaeaiiy. Iaoith ?iaioe ? neioac iiaeo a?ieia?/ii
aeoeaieo niieoe o ?yae? 3-cai?uaieo 4-a?ae?iene-2-ienio?iie?i?a oa ?o
iio?aeieo, a oaeiae aecia/aiiy iaea?eueo ia?niaeoeaieo c ieo aeey
iiaeaeueoiai ai?iaaaeaeaiiy ye iioaioe?eieo e?ea?nueeeo cania?a.

Aeey aeinyaiaiiy cacia/aii? iaoe aoee iinoaaeai? oae? caaea/?:

1. Cae?enieoe aeine?aeaeaiiy ?aaeoe?? oeeee?caoe?? aoeeiaiai ao??o
2-ea?aaoieneiaeiiai?eiai? eeneioe a oiiaao oa?iie?co.

2. ?ic?iaeoe i?aia?aoeai? niiniae iaea?aeaiiy oa cae?enieoe neioac
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a.

3. Iaea?aeaoe 4-I-aoeeeuei? iio?aei?
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a.

4. Aea/eoe ?aaeoe?th a?iioaaiiy 3-aee?e-,
3-ea?aaeeiene-4-a?ae?iene-2-ienio?iie?i?a oa
1-R-2,4-ae?ieni-3I-o?iie?i-3-ea?aiiiaeo eeneio.

5. Cae?enieoe neioac 5-R-1,3,4-o?aae?acie?e-2-ai?ae?a
1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio.

6. Aea/eoe o?ceei-o?i?/i? aeanoeaino? neioaciaaieo niieoe.

7. I?iaanoe a?ieia?/iee ne?ei?ia neioaciaaieo niieoe oa aeyaeoe aeaiaioe
aca?iica’yceo “no?oeoo?a oa?iaeieia?/ia ae?y”.

8. A?ae?a?aoe iaea?eueo ia?niaeoeaio o?i?/io no?oeoo?o aeey iiaeeaeaieo
oa?iaeieia?/ieo aeine?aeaeaiue.

Iaoeiaa iiaecia iaea?aeaieo ?acoeueoao?a. I?e aea/aii? iiaaae?iee
aoeeiaiai ao??o 2-ea?aaoieneiaeiiai?eiai? eeneioe a oiiaao oa?iie?co
aia?oa iieacaia iiaeeea?noue cae?eniaiiy eiiaeainaoe?? Ae?eiaia aac
aeei?enoaiiy iniiaieo eaoae?caoi??a. Iiaeaeueoa aeine?aeaeaiiy
cacia/aiiai o?i?/iiai ia?aoai?aiiy aeicaieeei ?ic?iaeoe i?aia?aoeaio
iaoiaeeeo neioaco 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a, yea aeaea
iiaeeea?noue iaea?aeoaaoe oe?eueia? i?iaeoeoe c aenieeie aeoiaeaie i?e
i?i?iaeueieo cao?aoao.

Anoaiiaeaii iniaeeaino? a?iioaaiiy
1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio, yea
noi?iaiaeaeo?oueny ?o aeaea?aieneethaaiiyi, ia iniia? /iai cai?iiiiiaaii
aoaeoeaiee neioac 1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?i?a.

Ca ?ic?iaeaieie iaoiaeeeaie neioaciaaia 71 iiaa niieoea, aoaeiaa oa
?iaeea?aeoaeuei?noue yeeo i?aeoaa?aeaeaia aeaiaioiei aiae?cii, iaoiaeaie
OO-, ?*-, II?-niaeo?ineii?? oa oiieioa?iai? o?iiaoia?ao??, a ie?aieo
aeiaaeeao – cono??/iei neioacii.

Aeine?aeaeaia aioeieneaeaioia, iaia?aiinoaa?e?coth/a, aioeoe?ai?aeia,
ae?o?aoe/ia, i?ioecaiaeueia, aioei?e?iaia, aioeeiaaoeyioia, aioe-A?E,
i?ioe?aeiaa, aa?a?oeeaeia oa ooia?oeeaeia aeoeai?noue neioaciaaieo
niieoe. Ca ?acoeueoaoaie aeine?aeaeaiiy a?ieia?/ii? aeoeaiino? aeyaeai?
ia?niaeoeai? niieoee c aioeieneaeaioiith, iaia?aiinoaa?e?coth/ith,
ae?o?aoe/iith oa ooia?oeeaeiith ae??th.

I?aeoe/ia cia/aiiy iaea?aeaieo ?acoeueoao?a. ?ic?iaeai? iaoiaee neioaco
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a oa
1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?i?a iiaeooue aooe aeei?enoai? i?e
neioac? iiaeo a?ieia?/ii aeoeaieo niieoe. Cie?aia, cai?iiiiiaaiee niin?a
iaea?aeaiiy 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a oni?oii canoiniao?oueny
a neioac? ?ioeo 3-cai?uaieo 4-a?ae?iene-2-ienio?iie?i?a.

?acoeueoaoe a?ieia?/iiai ne?ei?iao, a oaeiae anoaiiaeai? ie?ai?
caeiiii??iino? i?ae no?oeoo?ith oa a?ieia?/iith ae??th
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a, ?o 4-I-aoeeeueieo iio?aeieo,
3-a?ii-3-aee?e-2,4-ae?ienio?iie?i?a, 5-R-1,3,4-o?aae?acie?e-2-ai?ae?a
1-R-4-a?ae?iene-2-ieni-o?iie?i-3-ea?aiiiaeo eeneio iiiiaieee aaco
aeaieo, yea ? iniiaith iiaeaeueoiai oe?eani?yiiaaiiai iiooeo
iioaioe?eieo e?ea?nueeeo i?aia?ao?a na?aae iio?aeieo o?iie?io.

A yeino? ia?niaeoeaiiai aaiaoii?ioaeoi?iiai caniao aeey iiaeaeueoeo
iiaeeaeaieo aeine?aeaeaiue cai?iiiiiaaii
3-iii?e-4-a?ae?iene-2-ienio?iie?i, aeey yeiai ?ic?iaeaii i?iaeo
oei/aniai? oa?iaeiiaeii? noaoo?.

?ic?iaeai? iaoiaee neioaco, a oaeiae ?acoeueoaoe o?ceei-o?i?/ieo oa
oa?iaeieia?/ieo aeine?aeaeaiue ai?iaaaeaeaii a iaoeiai-aeine?aeio ?iaioo
oa a iaa/aeueiee i?ioean eaoaae?e oa?iaoeaaoe/ii? o?i?? Caii??aenueeiai
iaaee/iiai oi?aa?neoaoo oa aenia?eiaioaeueii? eaai?aoi??? CAI “A?IE?E”.

Iniaenoee aianie caeiaoaa/a:

– iaaaaeaia a aeena?oaoe?? aenia?eiaoaeueia neioaoe/ia /anoeia ?iaioe,
?*- oa OO-niaeo?aeuei? aeine?aeaeaiiy, a oaeiae ?ic?iaea i?iaeoo OON
aeeiiai? iniaenoi aaoi?ii;

– aiae?c, ia?iaea oa ioi?ieaiiy ?acoeueoao?a neioaoe/ieo,
o?ceei-o?i?/ieo oa a?ieia?/ieo aeine?aeaeaiue i?iaaaeai? aeena?oaioii.

Ai?iaaoe?y ?acoeueoao?a aeena?oaoe??. Iniiaiee ci?no aeena?oaoe?eii?
?iaioe aeiiia?aeaany ia ?anioae?eainuee?e iaoeiai-i?aeoe/i?e
eiioa?aioe?? “No/ani? i?iaeaie oa?iaoe??” (Oa?e?a, 1994); i?aeia?iaei?e
iaoeiai-i?aeoe/i?e eiioa?aioe?? “Nia?aiaiiua aniaeou nicaeaiey,
enneaaeiaaiey e ai?iaaoeee eaea?noaaiiuo n?aaenoa” (Oa?e?a, 1995); ia
iaoeiai-i?aeoe/i?e eiioa?aioe??, i?enay/ai?e 75-??//th Oe?OA
“Aeinyaiaiiy no/anii? oa?iaoe?? – a iaaee/io i?aeoeeo” (Oa?e?a, 1996).

Ioae?eaoe??. Iaoa??aee aeena?oaoe?? iioae?eiaai? o 5 noaooyo, 3 oacao
aeiiia?aeae oa 2 aeaiiiiaaieo ?oeiienao.

No?oeoo?a aeena?oaoe??. Aeena?oaoe?eia ?iaioa neeaaea?oueny c anooio,
o?ueio ?icae?e?a, aeniiae?a, nieneo e?oa?aoo?ieo aeaea?ae, aeiaeaoe?a.
Caaaeueiee ia’?i aeena?oaoe?? neeaaea? 132 noi??iee. ?iaioa ?ethno?iaaia
7 noaiaie, 3 iaethieaie ? 20 oaaeeoeyie. Ia?ae?e aeei?enoaieo
e?oa?aoo?ieo aeaea?ae i?noeoue 136 iaeiaioaaiue.

INIIAIEE CI?NO ?IAIOE

1. Neioac, o?i?/i? ia?aoai?aiiy oa a?ieia?/i? aeanoeaino? 3-

aee?ecai?uaieo 4-a?ae?iene-2-ienio?iie?i?a

Na?aae /eneaiieo i?e?iaeieo niieoe o?iie?iiai? no?oeoo?e iniaeeaee
?ioa?an aeeeeeathoue 3-aee?ecai?uai? 4-a?ae?iene-2-ienio?iie?ie, ye?
iathoue oe?ii? a?ieia?/i? aeanoeaino?, aea aea/ai? cian?i iaei.

Iaea?eueo iioe?ai? a?aeii? iaoiaee neioaco
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a iniiaai? ia aoeeethaaii? ai?e?i?a
aee?eiaeiiiaeie ao??aie c iaeii/aniith oa?i?/iith oeeee?caoe??th
ai?e?ae?a, ye? i?e oeueiio ooai?ththoueny, aai ia aoeeethaaii?
aee?eaio?ai?eao?a oei?aia?ae?eaeaie iiiiaoeeiaeo ao???a aee?eiaeiiiaeo
eeneio c ianooiiei caieeaiiyi o?iieiiiaiai oeeeeo ca Aeeeiaiii.

Iniiai? iaaeie?ee oeeo iaoiae?a iia’ycai? c ooai?aiiyi neiao?e/ieo
ae?ai?e?ae?a a ia?oiio aeiaaeeo oa iaeith aeinooii?noth aoeeethth/eo
aaaio?a a ae?oaiio. E??i oiai, a aeayeeo aeiaaeeao ia?oee iaoiae acaaae?
ia i?eaiaeeoue aei aaaeaieo ?acoeueoao?a. Aeoiaey/e c oeueiai, iaie aoee
c?iaeai? ni?iae oaeineiiaeaiiy iaoiae?a neioaco
3-aee?e-4-a?ae?iene-2-ienio?iie?i?a.

Oaea iiaeeea?noue c’yaeeanue a ?acoeueoao? aeine?aeaeaiiy ?aaeoe??
oa?iie?co ao???a 2-ea?aaeeieneiaeiiai?eiaeo eeneio (Noaia 1). Oae, i?ney
eei’yo?iiy aoeeiaiai ao??o 2-ea?aaoieneiaeiiai?eiai? eeneioe (1) a
aeeoai?eieneae? iaie aeae?eaii 2-ea?aaoieneai?e?ae
4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiai? eeneioe (2). sse a?aeiii, i??ie?c
aoeeiaeo ao???a iaeiiai?eiaeo eeneio aai ?o eei’yo?iiy a AeIOA
i?eaiaeeoue aei neiao?e/ieo ae?ai?e?ae?a. I/aaeaeii, a aeaiiio aeiaaeeo
ia?oith noaae??th ? ooai?aiiy ae?ai?e?aeo 3. Iaa?yae /e iiaeia iiynieoe
oeeee?caoe?th oe??? niieoee a o?iieii 2 a oiiaao oa?iie?co caeaoi?noth
iio?aeieo iaeiiiai? eeneioe ooai?thaaoe noaa?euei? ea?aai?iie,
ine?eueee, ii-ia?oa, aeo?aeiee ae?ao?? 1 oeeee?coaaany a a
4-a?ae?iene-3-ea?aaoiene-2-ienio?iie?i, a, ii-ae?oaa, eei’yo?iiy
ae?aoeeiaeiiaoo 4 c iaaeeeoeii aoeeaio?ai?eaoo 5 i?eaiaeeoue aei
ooai?aiiy eeoa ae?ai?e?aeo 3. ?ioeie neiaaie, iniiaieo aeanoeainoae
ai?iia?oie aoeeaio?ai?eaoo, eiia??i?noue ooai?aiiy yeiai iiaeia
i?eionoeoe a ?acoeueoao? oa?iie?co ae?ao??o 1, yaii iaaeinoaoiuei aeey
cae?eniaiiy oeeee?caoe?? ca oeiii ?aaeoe?? Ae?eiaia.

Noaia 1

wmetafile8? [email protected]??? ????????yyy????e

:???0????? ???? ???u??????????”????-????? ????
???u?????????”????-??????????E?4???4???Y?T???hT
??? ???? ???u??????????”????-?????????? ????
???u?????????”????-??????????4???*I??? ????
???u??????????”????-?????????? ????
???u?????????”????-??????????*I???l???°N???kJ
??? ???? ???u??????????”????-?????????? ????
???u?????????”????-??????????l???E?l??? ????
???u??????????”????-?????????? ????
???u?????????”????-??????????E?l???n?I???U?J???”?N
???n?I???E?4???E?l?????Oe??? ????
???u??????????”????-??????????u?y?????? Ana iaaaaeaia aeicaiey?
i?eionoeoe, ui aeaia ?aaeoe?y aeeth/a? noaae?th aioo??oiueiiieaeoey?ii?
aca?iiae?? a ?iieuei?e oi?i? 6, a ye?e ea?aii?euei?e aoii aoaeaoeth
neeaaeiiao??iiai oa?oioaaiiy aenooia? a ?ie? aeaeo?io?eo, a ?iie – ye
ioeeaio?e. Caieeaiiy o?iieiiiaiai oeeeeo 7, yea i?e oeueiio
a?aeaoaa?oueny, i?eaiaeeoue aei 2,4-ae?ieniiio?aeiiai 8 ? a e?ioeaaiio
?acoeueoao? – aei o?iieiio 2.

I?ii?aeia ooai?aiiy 2,4-ae?ienio?iie?io 8 iiaeia i?aeoaa?aeeoe ia
i?eeeaae? oa?iie?co N,N’-aee-2-ea?aaoieneai?e?aeo iaoeeiaeiiiai? eeneioe
12 (Noaia 2).

Noaia 2

wmetafile8? ?????? ????????yyy????c–???NO???? ????
???u??????????”????-????? ????
???u?????????”????-?????????????????*????*?
?? ???? ???u??????????”????-?????????? ????
???u?????????”????-??????????????Y??? ????
???u??????????”????-?????????? ????
???u?????????”????-??????????Y????B???o§???
??? ???? ???u??????????”????-?????????? ????
???u?????????”????-???????????B???B??? ????
???u??????????”????-?????????? ????
???u?????????”????-??????????B???°Y???
???Oe§???°Y??????B???I§??? ????
???u??????????”????-??????????u?y??????

A eeane/ieo oiiaao eiiaeainaoe?? Ae?eiaia iaei??th c i?ii?aeieo niieoe
oaeiae ? 2,4-ae?ieniiio?aeia 8, iaeiae a oeueiio aeiaaeeo aeey oiai, uia
?aaeoe?y iiaea eoe a iio??aiiio iai?yieo, iaiao?aeia iiaeeea?noue
ooai?aiiy ai?iio niieoee 10. Oaea ia?aoai?aiiy noi?iaiaeaeo?oueny
ae?i?ioaaiiyi i?ioiia (a ia eiai ia?aiinii, ye o aeiaaeeo oa?iie?co) ?
i?eaiaeeoue aei ai?iio 11, i?ney i?aeeeneaiiy yeiai aaea iiaea aooe
aeae?eaiee o?iieii 2.

Oaeei /eiii, iao? aeine?aeaeaiiy iieacaee iiaeeea?noue cae?eniaiiy
eiiaeainaoe?? Ae?eiaia ? i?e a?aenooiino? iniia, ui aeicaieeei
?icaeyiooe aeaio ?aaeoe?th c aeae?eueea ?ioi? oi/ee ci?o, yea
a?ae??ci??oueny a?ae ?? eeane/iiai iaaaaeaiiy.

Ne?ae cacia/eoe, ui ?icaeyiooa aeua ?aaeoe?y ooai?aiiy 3,3-aeecai?uaieo
2,4-ae?ienio?iie?i?a a ?acoeueoao? oa?iie?co neiao?e/ieo
aee-2-ea?aaeeieneai?e?ae?a aee?eiaeiiiaeo eeneio (Noaia 2) i?aaenoaaey?
oaeaeoa oai?aoe/iee ?ioa?an, i?ae i?aeoe/iee, ine?eueee ?? i?aeoe/ia
aeei?enoaiiy, ia aeaeue, aeineoue iaiaaeaia. A oie aea /an, iiaeaeueoa
?? aea/aiiy i?eaaei aei oe?eaai? neioaoe/ii? ciao?aeee.

sse aeyaeeinue, a i?enooiino? iniia, oiaoi a oiiaao eiiaeainaoe??
Ae?eiaia, N,N’-aee-2-ea?aaeeieneai?e?aee aee?eiaeiiiaeo eeneio (15) c
aenieeie aeoiaeaie ooai?ththoue a?aeiia?aei?
3-aee?e-4-a?ae?iene-2-ienio?iie?ie (14). Iaoai?ci ia?oeo aeaio noaae?e
caieeaiiy o?iieiiiaiai e?eueoey o aeaiiio aeiaaeeo aiaeia?/iee
oeeee?caoe?? ae?ai?e?aeo 3 (Noaia 1). Iiaeaeueoee aea ia?aa?a ?aaeoe??
ia? nai? iniaeeaino?, ine?eueee iaiao?aeia ia caaa?oaeuei?e noaae??
ooai?aiiy ai?iio e?ioeaaiai o?iieiio 15a iiaeeeaa eeoa o aeiaaeeo
a?aeuaieaiiy iaeiiai c cai?niee?a i?e aoii? aoaeaoeth a iieiaeaii? 3
niieoee 15a. Oaeei cai?nieeii aeyaeeinue ea?aai?e?aeia oa?oioaaiiy, yea,
i/aaeaeii o aeaeyae? o?aoaio, ? a?eueo eaaei iieeaeath/ei o?aaiaioii,
i?ae aee?eueiee cai?niee (Noaia 3).

Noaia 3

wmetafile8? ???!???????????yyy????th h?????ey??? ????
???u??????????”????-??
???u??????????”????-????ue???????????-????u??????1/4???I
”System?I???-????

????-????-?????.????u?y??????1/4???I???Times New Roman
Cyr?I???-????????2e:???15???-?????????'yy???-? ???-????? ???? ???u?????????"????-??????????????%;??? ???? ???u??????????"????-?????????? ???? ???u?????????"????-??????????p???%???…7???7 ??? ???? ???u??????????"????-?????????? ???? ???u?????????"????-??????????%??????? ???? ???u??????????"????-?????????? ???? ???u?????????"????-??????????????%O???X? ???-??? ???? ???u??????????"????-?????????? ???? ???u?????????"????-??????????%O???pO??? ???? ???u??????????"????-?????????? ???? ???u?????????"????-??????????pO??????? Ine?eueee neioac ae?ai?e?ae?a 15 iaaecae/aeii i?inoee, oi a oe?eiio aeaiee iaoiae iiaeia ?aeiiaiaeoaaoe ye i?aia?aoeaiee. Iaeei c eiai iaaeie?e?a — ia?aoe?iiaeueia aeei?enoaiiy aee?eaio?ai?eao?a. Iaeiae ? oeae iaaeie?e o a?eueoino? aeiaaee?a aaea?oueny onoiooe oeyoii i?aeai?o iaea?eueo iioeiaeueiiai ni?aa?aeiioaiiy ?aaaaio?a. sse a?aeiii, aoeeethaaiiy ai?e?i?a ae?aoeeiaeiiaoaie i?aeoe/ii caaaeaee noi?iaiaeaeo?oueny ooai?aiiyi neiao?e/ieo ae?ai?e?ae?a. E??i oiai, aenia?eiaioaeueii anoaiiaeaii, ui iaa?oue aeae?eai? a /enoiio aeaeyae? aoeeia? ao??e iaeiiai?eiaeo eeneio a aiaeia?/ieo oiiaao (iaa??aaiiy aei 170...200iN) eaaei ia?aoai?ththoueny a ae?ai?e?aee c ae?i?ioaaiiyi a?aeiia?aeieo ae?aoeeiaeiiao?a. A?aoiaoth/e oea, i?e aoeeethaaii? iaoeeaio?ai?eaoo 16 ae?aoeeiaeiiaoaie 17 c ieae/eie aee?eueieie cai?nieeaie aeioe?eueii aaiaeeoe a ?aaeoe?th iiaea?eiee iaaeeeoie aio?ai?eaoo. C iiaeiaaeaiiyi aoaeaaiaeiaaiai eaioethaeea aee?eueiiai cai?nieea aoeeethth/a caeaoi?noue ae?oai? aoieneea?aii?eueii? a?oie iaeiiiaeo ao???a 17 iaaea? iano?eueee (i/aaeaeii, aiane?aeie noa?e/ieo ia?aoeiae), ui caaeia?euei? ?acoeueoaoe iiaeia iaea?aeaoe aaea ? i?e aea?iiey?ieo ni?aa?aeiioaiiyo ao???a 16 oa 17. sse ua iaeei iiceoeaiee iiiaio ne?ae a?aei?oeoe oa, ui aeaiee niin?a ia iio?aao? ?icae?eaiiy iiii- ? ae?ai?e?ae?a aee?eiaeiiiaeo eeneio 18 oa 15, ye? a ??cieo ni?aa?aeiioaiiyo caaaeaee i?enooi? a ?aaeoe?ei?e noi?o? (Noaia 4). Noaia 4 wmetafile8? ????? ?????????yyy????a???Oa??? ???? ???u??????????"????-?????u?y?????? 14 R = H: a R = CH3; a R = C2H5; a R = CH2CH=CH2; a R = C3H7; ae R = i-C3H7; a R = C4H9; ae R = C5H11; c R = C6H13; e R = C7H15; e R = C8H17; e C9H19; i R = C10H21; i R = C12H25; i R = CH2C6H5; R = CH3; i R = C4H9 Cia/ii ?icoe?th? iiaeeeaino? iaoiaeo aeei?enoaiiy ye aoeeethth/eo aaaio?a aeinooiieo aeeoei?aia?ae?eae?a aee?eiaeiiiaeo eeneio 20, yea aeicaiey? eaaei neioacoaaoe ye 1I-3-aee?e-4-a?ae?iene-2-ienio?iie?ie 14a-i, oae ? ?o 1-cai?uai? aiaeiae 14i. O?i?/ia aoaeiaa 3-aee?ecai?uaieo 4-a?ae?iene-2-ienio?iie?i?a 14 i?aeoaa?aeaeaia aeaiaioiei aiae?cii oa aeaieie II?- ? OO-niaeo?ineii??. Iaeiei c iaoiae?a noai?aiiy iiaeo e?ea?nueeeo cania?a, ye a?aeiii, ? neioac i?ie?e?a, oiaoi o?i?/ia iiaeeo?eaoe?y a?aeiiiai i?aia?aoo c o??th /e ?ioith iaoith: iineeaiiy aeoeaiino?, iiaeiaaeaiiy o?eaaeino? ae??, cieaeaiiy oiene/iino?, onoiaiiy iai?e?iiiai niaeo oa ?io. Aeei?enoiaoth/e oeae i?eioeei, c iaoith aeyaeaiiy caeiiii??iinoae ca’yceo “o?i?/ia aoaeiaa — a?ieia?/ia aeoeai?noue” iaie iaea?aeai? 4-I-aoeeeuei? iio?aei? 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a 22. Neioac cae?eniaii aoeeethaaiiyi 4-a?ae?ieneiio?aeieo 14 aia?ae?eaeaie /e oei?aia?ae?eaeaie ea?aiiiaeo eeneio: Noaia 5 wmetafile8? ??&??? ????????yyy????yr????.??? ???? ???u??????????"????-?????u?y?????? 22 a Alk = i-Pr, R = Me; a Alk = Pr, R = Et; a Alk = Pr, R = CH2CH2COOMe; a Alk = Bu, R = Me; ae Alk = Bu, R = CH2Cl; a Alk = i-Bu, R = Me; ae Alk = NH2-Ph, R = Me; c Alk = NH2-Ph, R = Ph; e Alk = NH2-Ph, R = C15H31 I?iaeiaaeoth/e aeine?aeaeaiiy ii iiooeo iioaioe?eieo aioei?e?iaieo e?ea?nueeeo cania?a na?aae aaei?aecai?uaieo o?iie?i?a, iaie aea/aia iiaaae?iea 3-cai?uaieo 4-a?ae?iene-2-ienio?iie?i?a a oiiaao a?iioaaiiy iieaeoey?iei a?iiii (Noaia 6). I?e oeueiio anoaiiaeaii, ui a eueiaeyi?e ioeoia?e eeneio? 3-aee?ecai?uai? 4-a?ae?iene-2-ienio?iie?ie (14) eaaei ooai?ththoue 3-a?ii-3-aee?e-2,4-ae?ienio?iie?ie 23 c aenieeie aeoiaeaie. sse ? ne?ae aoei /aeaoe, ia?iaea inoaii?o iaoeeaoii iao??th aea? 3-iaoieneiio?aei? 24, oiae? ye o?ao-aooeeao eae?th aeeeeea? oaeaeea aeaa?ae?ia?iioaaiiy c ooai?aiiyi aeo?aeieo 3-aee?eo?iie?i?a 14. Ne?ae cacia/eoe oe?eaao iiaaae?ieo a oiiaao aeine?aeaeoaaii? ?aaeoe?? 1-R-2,4-ae?ieni-3I-o?iie?i-3-ea?aiiiaeo eeneio (25). sseui aoeeia? ao??e 26, iiae?aii aei 3-aee?eo?iie?i?a 14, ooai?ththoue a?aeiia?aei? 3-a?ii-2,4-ae?ieniiio?aei? 27, oi i?ney ia?iaee a?iiii eeneio 25 c ?aaeoe?eii? noi?o? aeae?eai? 1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?ie 28, aoaeiaa yeeo i?aeoaa?aeaeaia cono??/iei neioacii, a naia eeneioiei a?ae?ie?cii ao???a 27. Neeueii ae?aaeai? eeneioi? aeanoeaino?, a ioaea ? eaae?noue aeaea?aieneethaaiiy 3-a?ii-2,4-ae?ienio?iie?i-3-ea?aiiiaeo eeneio 29, ye? nii/aoeo ooai?ththoueny, iiaeia iiynieoe aeae?eueeiia oaeoi?aie. Ii-ia?oa, iiaeeea?noth noaa?e?caoe?? ai?ii?a eeneio 25 ca ?aooiie aeaeieae?caoe?? ?o ca?yae?a oeyoii ooai?aiiy aioo??oiueiiieaeoey?ieo aiaeiaaeo ca’yce?a ca oeiii i?oi-aoaeoa o i-a?ae?iene- ?, iniaeeai, i-aeea?ae?ieneaaicieieo eeneio. I/aaeaeii, naia oeei oaeoi?ii iiynith?oueny eaea?noue ai?aeoaaiiy 1-R-2,4-ae?ieni-3I-o?iie?i-3-ea?aiiiaeo eeneio. Ii-ae?oaa, aaaaeaiiy aeaeo?iiiaeoeaioi?iiai cai?nieea (aoiia a?iio) a -iieiaeaiiy ii a?aeiioaiith aei ea?aieneeueii? a?oie coiiaeth? ua a?eueo nooo?aa i?aeaeuaiiy eeneioiino?. Eiia??ii, ii?aeiaiiy cacia/aieo aoaeo?a ? i?ecaiaeeoue aei oiai, ui a?iicai?uai? eeneioe 29 aeaea?aieneeththoueny aaea i?e e?iiaoi?e oaiia?aoo??. A?aoiaoth/e i?inoioo neioaco 1-R-2,4-ae?ieni-3I-o?iie?i-3-ea?aiiiaeo eeneio 25 oa aeaaeea i?io?eaiiy ?o a?iioaaiiy, aeaiee iaoiae iiaeia ?aeiiaiaeoaaoe ye i?aia?aoeaiee aeey iaea?aeaiiy 1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?i?a (28). An? iaaaaeai? ia noai? 6 a?iicai?uai? o?iieiie yaeythoue niaith na?oei-aeiao? e?enoae?/i? ?a/iaeie c /?oeeie oaiia?aoo?aie ieaaeaiiy, i?aeoe/ii ia?ic/eii? o aiae? oa aeia?a ?ic/eii? a a?eueoino? i?aai?/ieo ?ic/eiiee?a. ?o o?i?/ia aoaeiaa i?aeoaa?aeaeaia ye aeaiaioiei aiae?cii, oae ? niaeo?aeueieie iaoiaeaie. Iacaaaeath/e ia oe?iea ?iciianthaeaeaiiy o i?e?iae?, 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a eeoa a iaaaaaoueio ioae?eaoe?yo iaaiaeyoueny a?aeiiino? i?i aea/aiiy ?o a?ieia?/ieo aeanoeainoae, i?e/iio /ano?oa o?eueee i?i aioei?e?iaio oa ooia?oeeaeio aeoeai?noue. Aeoiaey/e c oeueiai, neioaciaai? iaie 3-aee?e-4-a?ae?iene-2-ienio?iie?ie 14 aoee i?aeaeai? oa?iaeieia?/iiio ne?ei?iao ia aeyaeaiiy aioeoe?ai?aeii?, i?ioecaiaeueii?, aioei?e?iaii?, iaia?aiinoaa?e?coth/i? ? aioeieneaeaioii? aeoeaiino?. Aea/aii oaeiae aieea oeeo ?a/iaei ia aeae?eueio ooieoe?th ie?ie oa nenoaio cn?aeaiiy e?ia?. A?aoiaoth/e iniaeeao aeooaeuei?noue iiooeo oa noai?aiiy e?ea?nueeeo i?aia?ao?a, i?eaeaoieo aeey e?eoaaiiy NI?Aeo ? iieieia?/ieo caoai?thaaiue, aeaye? c neioaciaaieo iaie ?a/iaei i?ieoee ia?aa??eo ye iioaioe?ei? aioe-A?E ? i?ioe?aeia? aaaioe. Noaia 6 wmetafile8? ??“%???????????yyy????3/4d???·“???? ???? ???u??????????"????-?????u?y?????? 14, 23 a R = CH3, a R = C2H5, a R = C3H7, a R = C4H9, ae R = C5H11, a R = C6H13, ae R = C7H15, c R = C8H17, e R = CH2C6H5; 26, 27 a R = H, a R = CH3, a R = C2H5; 25, 28 a R = CH3, a R = C2H5, a R = C6H13 sse aeyaeeinue, niieoee 14a-i i?iyaeththoue aenieo aioeieneaeaioio aeoeai?noue ? a a?eueoino? aeiaaee?a aeinoia??ii ia?aaeuothoue i?aia?ao ii??aiyiiy (a?oai?i A). Ae?aaeaia iaia?aiinoaa?e?coth/a ae?y niinoa??aaeanue aeey niieoe 14a,ae,e, ye? ia?aaeuothoue aeoeai?noue nee?ai?o, a niieoee 14ae,a,i ae?thoue ia ??ai? inoaiiueiai. Ne?ae cacia/eoe, ui niieoee 14e,ae,?,a aeyaeythoue i?e oeueiio ua e aenieo aioeieneaeaioio ae?th. Oe?eaaa oaiaeaioe?y i?iaeyaea?oueny i?e aea/aii? o?iieii?a 14 ia na/iaeae?eueio ooieoe?th ie?ie. Aeyaeeinue, ui ?a/iaeie, ye? i?noyoue ia?io e?euee?noue aoii?a aoaeaoeth a aee?eueiiio cai?nieeo (14a,c,i), i?iyaeythoue ae?aaeaio na/ia?iio ae?th, eeoa aeaui iinooiath/enue a?iio?aceaeo. A oie aea /an, o?iieiie c iaia?iei /eneii aoiiia aoaeaoeth a aee?eueieo eaioethaeeao ca ??aeeei aeeeth/aiiyi aai acaaae? ia aieeaathoue ia na/iaeae?eaiiy, aai ae aeeeeeathoue neeueia cieaeaiiy ae?o?aco, ia?aaaaeath/e ca aeoeai?noth (iai?eeeaae, o?iieii 14ae) aioeae?o?aoe/iee ai?iii aae?o?ae?ei. Ae?aaeaia aioeeiaaoeyioa ae?y o ii??aiyii? n oai?iia?iiii niinoa??aaeanue o 3-aaicee-4-a?ae?iene-2-ienio?iie?io (14i). Uiaei ?ioeo a?ieia?/ieo aei?iaoaaiue 3-aee?e-4-a?ae?iene-2-ienio?iie?ie 14, oi aiie iieacaee, ui oe? niieoee aeyaeythoue neaaeiae?aaeaio aioeoe?ai?aeio aeoeai?noue; i?aeoe/ii iaaeoeaieie aiie aeyaeeenue i?e aeine?aeaeaii? i?ioecaiaeueii?, aioei?e?iaii?, aioe-A?E oa aioe?aeiai? ae??. Aeey 4-I-aoeeeueieo cai?uaieo 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a (22) aoea aeine?aeaeaia aioeieneaeaioia, iaia?aiinoaa?e?coth/a, ae?o?aoe/ia ? i?ioecaiaeueia aeoeai?noue. sse ? o aeiaaeeo niieoe 14, iaea?eueo aoaeoeaieie ?o 4-I-aoeeeuei? aiaeiae aeyaeeeny a ieai? i?iyaeaiiy aiioeieneaeaioii? oa iaia?aiinoaa?e?coth/i? ae??. I?e oeueiio, iaea?eueo aeniea iaia?aiinoaa?e?coth/a aeoeai?noue, yea ia?aaeuoa ??aaiue nee?ai?o, yiinoa??aaeany o ?a/iaei, ye? i?noyoue caeeoie ioeoiai? (22a,a) aai oei?ioeoiai? (22ae) eeneio. Ca?eueoaiiy e?eueeino? aoii?a aoaeaoeth a aoeeeueiiio o?aaiaio? i?ecaiaeeoue aei cieaeaiiy iaia?aiinoaa?e?coth/i? aeoeaiino?, a aaaaeaiiy caeeoeo aeeea?aiiiai? eeneioe (22a) - ia o?eueee aei iiaii? ?? ao?aoe, a e aei i?aeaeuaiiy eiioeaio?aoe??? AeAO. A?aei?/aia iaie ?ai?oa aeey 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a (14) caeaaei?noue na/iaea?aeii? ae?? a?ae e?eueeino? aoii?a aoaeaoeth a aee?eueiiio caeeoeo, ia i?inoaaeo?oueny o ?o 4-I-aoeeeueieo iio?aeieo 22, ye? aeyaeythoue ae?aaeaio ae?o?aoe/io ae?th, yea, iaeiae, ia ia?aaeuo? i?aia?ao ii??aiyiiy - a?iioeaceae. Aeine?aeaeaiiy i?ioecaiaeueii? aeoeaiino? niieoe 22, iieacaei, ui, ia aeaeue, aeey 4-I-aoeeeueieo iio?aeieo 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a i?ioecaiaeueia aeoeai?noue ia oa?aeoa?ia. Aeey 3-a?ii-3-aee?e-2,4-ae?ienio?iie?i?a (23) aoei aeine?aeaeaii aioei?e?iaio aeoeai?noue, yeo iiaeia ioa?aeoa?ecoaaoe ye neaaiae?aaeaio. Oaeei /eiii, i?iaaaeai? oa?iaeieia?/i? aeine?aeaeaiiy a?aee?eaathoue ia?niaeoeao noai?aiiy iiaeo e?ea?nueeeo i?aia?ao?a ia iniia? iio?aeieo 4-a?ae?iene-2-ienio?iie?i?a. Cie?aia, 3-iii?e-4-a?ae?iene-2-ienio?iie?i (14e), yeee aeyaey? aenieo iaia?aiinoaa?e?coth/o oa aioeieneaeaioio aeoeai?noue, ?aeiiaiaeiaaiee aeey iiaeeaeaieo oa?iaeieia?/ieo aeine?aeaeaiue ye iioaioe?eiee aaiaoii?ioaeoi?iee can?a, a ca’yceo c /ei iaie ?ic?iaeaii i?iaeo oei/aniai? oa?iaeiiaeii? noaoo? ia oeth ?a/iaeio. 2. Neioac, o?ceei-o?i?/i? oa a?ieia?/i? aeanoeaino? 5-R-1,3,4-o?aae?a- cie?e-2-ai?ae?a 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio Noai?aiiy oa ai?iaaaeaeaiiy a iaaee/io i?aeoeeo iiaeo aoaeoeaieo aioeaaeoa??aeueieo cania?a caaea/a, yea iino?eii iio?aao? ae??oaiiy, caaaeath/e ia iiyao i?ae aieeaii /ano iiaeo no?eeeo ooai?a iaoiaaiii? i?e?ioei?e. A ?acoeueoao? aeine?aeaeaiue, i?iaaaeaieo ?ai?oa ia eaoaae?? oa?iaoeaaoe/ii? o?i?? Oe?a?inueei? oa?iaoeaaoe/ii? aeaaeai??, aeineoue aeniea aioei?e?iaia aeoeai?noue aoea aeyaeaia o iio?aeieo 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio oa 1,3,4-o?aae?acieo. Ia’?aeiaiiy a iaei?e iieaeoe? oaeeo aeoeiaeo o a?ieia?/iiio a?aeiioaii? no?oeoo? ye N-aee?e-4-a?ae?ieneo?iie?i-3-ea?aiiia? eeneioe ? 5-R-1,3,4-o?aae?aciee noai?th? ?aaeuei? ia?aaeoiiae aeey neioaco aoaeoeaieo oa?iaeieia?/ieo cania?a, ui ? iineoaeeei oai?aoe/iei iaa?oiooaaiiyi aeine?aeaeaiue o oeueiio iai?yieo. Ai?aee 31a-y aoee iaea?aeai? oa?iie?cii aea?iiey?ieo e?eueeinoae aoeeiaeo ao???a 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio 26 ? 2-ai?ii-5-R-1,3,4-o?aae?acie?a 30 o a?aeiia?aeiino? aei iaoiaeeee, ?ic?iaeaii? iaie ?ai?oa, ca noaiith 7. Neioaciaai? niieoee yaeythoue niaith aacaa?ai? e?enoae?/i? ?a/iaeie c /?oeeie oaiia?aoo?aie ieaaeaiiy, i?aeoe/ii ia?ic/eii? o aiae? oa a?eueoino? i?aai?/ieo ?ic/eiiee?a. Aioei?e?iaio aeoeai?noue iaea?aeaieo niieoe aecia/aee ii a?aeiioaiith aei oaeeo oano-ooai?a: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 25853) ? Bacillus subtilis (ATCC 66330). Aeine?aeaeaiiy iieacaee, ui c 20 ia?aa??aieo niieoe aioei?e?iaio aeoeai?noue ii a?aeiioaiith aei ??cieo ooai?a i?e?ii?aai?ci?a o eiioeaio?aoe?? 31,25- Noaia 7 wmetafile8? ?? ???????????yyy????ma???aeO???? ???? ???u?????????"????-?????X31 R= H: a R = H; a R = Me; a R = Et; a R = Pr; ae R = i-Pr; a R = Bu; ? R = i-Bu; ae R = SO2NH2 R = Me c R = H; e R = Me; ? R = Et; e R = Pr; e R = i-Pr; i R = Bu; i R = SO2NH2 R = Et i R = H; i R = Me; ? R = Et; n R = Pr; o R = i-Pr; o R = Bu; o R = SO2NH2 R = Pr o R = H; oe R = Me; / R = Et; o R = Pr; u R = i-Pr; th R = Bu; y R = SO2NH2 62,5 iea/ie i?iyaeee 7 ?a/iaei, i?e/iio niieoea 31o aeyaeeany aeoeaiith ii a?aeiioaiith aei an?o aeei?enoaiieo oano-ooai?a. Ne?ae cacia/eoe, ui ca oeiii aioei?e?iaii? ae?? an? aeine?aeaeoaai? niieoee ? aaeoa??inoaoeeaie. Aiae?coth/e ?acoeueoaoe aeine?aeaeaiue, iiaeia c?iaeoe aeniiaie, ui aecia/aeueieie oaeoi?aie i?iyaeaiiy aea??eiai? aioei?e?iaii? aeoeaiino? ? iayai?noue ?icaaeoaeaiiai aee?eueiiai cai?nieea a iieiaeaii? 5 o?aae?acieueiiai oeeeeo. A oie aea /an i?enooi?noue N1-N4 aee?eueieo cai?niee?a a iieiaeaii? 1 o?iie?iiaiai oeeeeo ?noioiiai aieeao ia aioei?e?iaio ae?th ia ia?. Aea/aiiy aa?a?oeeaeii? aeoeaiino? niieoe 31 ia aeyaeei aeoeaieo a oeueiio ieai? ?a/iaei. A?eueo aoaeoeaii o?aae?acie?e-2-ai?aee 1-R-4-a?ae?iene-2-ieni-o?iie?i-3-ea?aiiiaeo eeneio (31) iiaeooue aooe canoiniaai? ye ooia?oeeaee. Iniaeeai aeoeaieie aeaye? c aeine?aeaeaieo ?a/iaei, a naia 31a,?,u, aeyaeeenue o ai?iouea? c eenoeiaith ??aeath, ie?eeoey??icii ?eno oa ieyieno?noth eieineiai? eonee ioaieoe?, ui a?aee?eaa? ia?niaeoeao noai?aiiy ia iniia? o?aae?acie?e-2-ai?ae?a 1-R-4-a?ae?iene-2-ieni-o?iie?i-3-ea?aiiiaeo eeneio (31) iioaioe?eieo ooia?oeeae?a aeey n?euenueeiai ainiiaea?noaa. AENIIAEE 1. Aia?oa iieacaia iiaeeea?noue cae?eniaiiy eiiaeainaoe?? Ae?eiaia a oiiaao, a?aei?iieo a?ae eeane/ieo — i?e a?aenooiino? iniiaieo eaoae?caoi??a; cai?iiiiiaaii eiia??iee iaoai?ci oeueiai o?i?/iiai ia?aoai?aiiy. 2. Cae?eniaii neioac a?ieia?/ii aeoeaieo ?a/iaei a ?yae? 3-cai?uaieo a?ae?iene(ieni)o?iie?i?a: 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a; 4-I-aoeee-3-aee?e-4-a?ae?iene-2-ienio?iie?i?a; 3-a?ii-3-aeeee-2,4-ae?ienio?iie?i?a; 5-R-1,3,4-o?aae?acie?e-2-ai?ae?a 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio. 3. ?ic?iaeaii i?aia?aoeaiee niin?a iaea?aeaiiy 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a. I?e oeueiio ?aoe?iiaeueia aeei?enoaiiy aeo?aeieo aee?eaio?ai?eao?a aeinyaa?oueny oeyoii i?aeai?o iioeiaeueiiai ni?aa?aeiioaiiy ?aaaaio?a a caeaaeiino? a?ae no?oeoo?e aee?eueiiai cai?nieea. Cai?iiiiiaaiee iaoiae ciaeoia canoinoaaiiy a i?aai?/i?e o?i?? oeyoii iioe?aiiy ia neioac ?ioeo 3-cai?uaieo 4-a?ae?iene-2-ienio?iie?i?a. 4. Cae?eniaii ia?aoai?aiiy 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a a oiiaao ?aaeoe?e aoeeethaaiiy oa a?iioaaiiy. 5. Cai?iiiiiaaii i?inoee oa aoaeoeaiee neioac 1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?i?a, yeee cae?enith?oueny a?iioaaiiyi 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio, yea noi?iaiaeaeo?oueny aeaea?aieneethaaiiyi inoaii?o. 6. Oa?iaeieia?/i? aei?iaoaaiiy neioaciaaieo niieoe na?ae/aoue i?i ia?niaeoeai?noue iiooeo na?aae aeine?aeaeoaaieo o?iie?i?a a?ieia?/ii aeoeaieo ?a/iaei c aenieith aioeieneaeaioiith, iaia?aiinoaa?e?coth/ith, ae?o?aoe/iith, aioeeiaaoeyioiith oa aioei?e?iaiith ae??th. Aeoiaey/e c ii??aiyeueii? ioe?iee oa?iaeieia?/ii? aeoeaiino? iaea?eueo aoaeoeaieo na?aae canoiniao?ieo o iaaee/i?e i?aeoeoe? i?aia?ao?a oa iiaeo neioaciaaieo niieoe, aeey iiaeeaeaieo oa?iaeieia?/ieo aeine?aeaeaiue cai?iiiiiaaii 3-iii?e-4-a?ae?iene-2-ienio?iie?i ye iioaioe?eiee aaiaoii?ioaeoi?iee can?a. ?ic?iaeaii i?iaeo OON ia oeth niieoeo. 7. Anoaiiaeaii ?yae caeiiii??iinoae ca’yceo “no?oeoo?a — ae?y”, ye? iiaeooue aooe aeei?enoai? aeey oe?eani?yiiaaiiai iiooeo ?a/iaei c iaia?aiinoaa?e?coth/ith, ae?o?aoe/iith oa aioei?e?iaiith ae??th. 8. Ca ?acoeueoaoaie aei?iaoaaiue aa?a?oeeaeii? oa ooia?oeeaeii? aeoeaiino? 5-R-1,3,4-o?aae?acie?e-2-ai?ae?a 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio aeyaeaii ?a/iaeie, aeoeai? ii a?aeiioaiith aei oaeeo caoaeiee?a oai?ia n?euenueeiainiiaea?nueeeo eoeueoo? ye eenoeiaa ??aea, ie?eeoey??ic ?eno oa ieyieno?noue eieineiai? eonee ioaieoe?. Iaea?aeai? ?acoeueoaoe a?aee?eaathoue ia?niaeoeao noai?aiiy ia iniia? aeine?aeaeoaaieo niieoe iioaioe?eieo ooia?oeeae?a aeey n?euenueeiai ainiiaea?noaa. Nienie iioae?eiaaieo i?aoeue ca oaiith aeena?oaoe??: 1. 4-Ieneoeiieiiu-2. 15. Neioac -(ie?eaeee-2)-aieaeia 1--4-aeae?iene-2-oeiieii-3-ea?aiiiauo eeneio eae aiciiaeiuo iiauo ianoa?ieaeiuo i?ioeaiainiaeeoaeueiuo n?aaenoa / E.A.Oe?aeiaoe, N.A.Oa?ai, I.A.Aaoeoaaaa, A.A.Oo?ia // Oeiey aaoa?ioeeee. niaaeeiaiee. — 1993. — ? 8. — N. 1101-1104. 2. 4-Ieneoeiieiiu-2. 17. Eiiaeainaoeey Ae?eiaia eae oa?ie/anee aeoeae?iaaiiue i?ioeann / E.A.Oe?aeiaoe, N.A.Oa?ai, I.A.Aacoaeue, I.A.Aaoeoaaaa // Oeiey aaoa?ioeeee. niaaeeiaiee. — 1993. — ? 9. — N. 1219-1222. 3. 4-Ieneoeiieiiu-2. 19. Iiaue neioac 3-aeeee-2-ieni-4-aeae?ieneoeiieeiia / E.A.Oe?aeiaoe, N.A.Oa?ai, I.A.Aaoeoaaaa, I.A.Ai?ioiaa, A.A.Oo?ia, E.I.Ai?iieia, I.E.Oeeeiiiiaa // Oeiey aaoa?ioeeee. niaaeeiaiee. — 1994. — ? 5. — N. 673-678. 4. 4-Ieneoeiieiiu-2. 22. Neioac e aeieiae/aneea naienoaa 1-aeeee(a?ee)-2-ieni-3-ea?ayoiene-4-aeae?ieneoeiieeiia e eo i?iecaiaeiuo / E.A.Oe?aeiaoe, I.A.Ai?ioiaa, N.A.Oa?ai, I.A.Aacoaeue, A.A.Oo?ia, I.A.Ia?onaiei, I.A.Aaoeoaaaa // Oeiey aaoa?ioeeee. niaaeeiaiee. — 1994. — ? 7. — N. 958-966. 5. 4-Ieneoeiieiiu-2. 26. A?iie?iaaiea 3-caiauaiiuo 2-ieni-4-aeae?ieneoeiieeiia / E.A.Oe?aeiaoe, N.A.Oa?ai, I.A.Aaoeoaaaa, I.A.Ai?ioiaa, I.E.Oeeeiiiiaa, A.A.Oo?ia // Oeiey aaoa?ioeeee. niaaeeiaiee. — 1995. — ? 2. — N. 204-207. 6. Neioac e i?ioeaiiee?iaiay aeoeaiinoue 5--1,3,4-oeaaeeacieee-2-aieaeia 1-aeeee-2-ieni-4-aeae?ieneoeiieei-3-ea?aiiiauo eeneio / E.A.Oe?aeiaoe, N.A.Oa?ai, I.A.Aaoeoaaaa, E.E.Aeeeee, I.E.Oeeeiiiiaa // Oe?aeineay oa?iaoe. aeaaeaiey, Oa?ueeia, 1994. — 10 n.: Aeaeeia?ao.: 7 iaca. — ?on. — Aeai. a AIOA Oe?aeiu 10.05.95. — ? 1061-Oe-95 7. Aeieiae/aneea naienoaa 3-aeeee-2-ieni-4-aeae?ieneoeiieeiia / N.A.Oa?ai, I.A.Aaoeoaaaa, I.A.Ai?ioiaa, E.A.Oe?aeiaoe, E.I.Ai?iieia, A.I.E?aa/aiei, I.E.Oeeeiiiiaa // Oe?aeineay oa?iaoe. aeaaeaiey, Oa?ueeia, 1995. — 9 n.: Aeaeeia?ao.: 11 iaca. — ?on. — Aeai. a AIOA Oe?aeiu 12.07.95. — ? 1806 - Oe-95 ?ao?o??aa I.A. “Neioac, o?ceei-o?i?/i? oa a?ieia?/i? aeanoeaino? 3-cai?uaieo 4-a?ae?iene-2-ienio?iie?i?a”. - ?oeiien. Aeena?oaoe?y ia caeiaoooy iaoeiaiai nooiaiy eaiaeeaeaoa oa?iaoeaaoe/ieo iaoe ca niaoe?aeuei?noth 15.00.02 - oa?iaoeaaoe/ia o?i?y ? oa?iaeiaiic?y. - Oe?a?inueea oa?iaoeaaoe/ia aeaaeai?y, Oa?e?a, 1999. Iaea?aeaii iia? a?ieia?/ii aeoeai? niieoee a ?yae? 3-cai?uaieo a?ae?iene(ieni)o?iie?i?a: 3-aee?e-4-a?ae?iene-2-ienio?iie?ie oa ?o 4-I-aoeeeuei? iio?aei?; 3-a?ii-3-aee?e-2,4-ae?ienio?iie?ie; 5-R-1,3,4-o?aae?acie?e-2-ai?aee 1-R-4-a?ae?iene-2-ienio?iie?i-3-ea?aiiiaeo eeneio. ?ic?iaeaii i?aia?aoeai? iaoiaeeee neioaco 3-aee?e-4-a?ae?iene-2-ienio?iie?i?a ? 1-R-3-a?ii-4-a?ae?iene-2-ienio?iie?i?a. Aia?oa iieacaia iiaeeea?noue cae?eniaiiy eiiaeainaoe?? Ae?eiaia a oiiaao oa?iie?co, yea a?aeaoaa?oueny ia a?aei?io a?ae eeane/ieo oyaeaiue i?e a?aenooiino? iniiaieo eaoae?caoi??a; cai?iiiiiaaii eiia??iee iaoai?ci oeueiai ia?aoai?aiiy. Aea/ai? OO-, ?*- oa II? niaeo?aeuei? oa?aeoa?enoeee neioaciaaieo ?a/iaei. Ca ?acoeueoaoaie oa?iaeieia?/iiai ne?ei?iao aeyaeai? aoaeoeai? niieoee iaia?aiinoaa?e?coth/i?, aioeieneaeaioii?, ae?o?aoe/ii?, aioeeiaaoeyioii? oa ooia?oeeaeii? ae??; anoaiiaeai? ie?ai? caeiiii??iino? ca’yceo “aoaeiaa — ae?y”. Iaea?eueo ia?niaeoeaia niieoea ?aeiiaiaeiaaia ye iioaioe?eiee aaiaoii?ioaeoi?iee can?a. Eeth/ia? neiaa: 4-a?ae?iene-2-ienio?iie?i, aee?eaio?ai?eaoe, neioac, oa?iie?c, aaoa?ioeeee?caoe?y, aaiaoii?ioaeoi?iee can?a. Aaoeoaaaa I.A. “Neioac, oeceei-oeie/aneea e aeieiae/aneea naienoaa 3-caiauaiieo 4-aeae?iene-2-ienioeiieeiia”. - ?oeiienue. Aeenna?oaoeey ia nieneaiea o/aiie noaiaie eaiaeeaeaoa oa?iaoeaaoe/aneeo iaoe ii niaoeeaeueiinoe 15.00.02 - oa?iaoeaaoe/aneay oeiey e oa?iaeiaiicey. - Oe?aeineay oa?iaoeaaoe/aneay aeaaeaiey, Oa?ueeia, 1999 a. Aeenna?oaoeey iinayuaia iieneo iioaioeeaeueiuo eaea?noaaiiuo n?aaenoa a ?yaeo 3-caiauaiiuo 4-aeae?iene-2-ienioeiieeiia. N yoie oeaeueth inouanoaeai neioac 3-aeeee-4-aeae?iene-2-ienioeiieeiia e eo 4-I-aoeeeueiuo i?iecaiaeiuo; 3-a?ii-3-aeeee-2,4-aeeienioeiieeiia; 5-R-1,3,4-oeaaeeacieee-2-aieaeia 1-R-4-aeae?iene-2-ienioeiieei-3-ea?aiiiauo eeneio. Caaea/a oniaa?oainoaiaaiey nouanoaothueo iaoiaeia neioaca 3-aeeeecaiauaiiuo 4-aeae?iene-2-ienioeiieeiia auea ?aaeeciaaia a ?acoeueoaoa enneaaeiaaiey ?aaeoeee oeeeeecaoeee yoe?ia 2-ea?aaeeieneiaeiiaieeiauo eeneio. Eae ieacaeinue, a oneiaeyo oa?iieeca oeacaiiua yoe?u ia?acotho 2-ea?aaeeieneaieeeaeu 4-aeae?iene-2-ienioeiieei-3-ea?aiiiauo eeneio, /oi aeieacuaaao aiciiaeiinoue inouanoaeaiey eiiaeainaoeee Aeeeiaia, a ioee/ea io eeanne/aneeo i?aaenoaaeaiee, i?e ionoonoaee iniiaiuo eaoaeecaoi?ia. Aa?iyoii, aeaiiay ?aaeoeey aeeth/aao noaaeeth aioo?eiieaeoey?iiai acaeiiaeaenoaey a aiieueiie oi?ia i?iiaaeooi/iiai N,N-aee-2-ea?aaeeieneaieeeaea iaeiiiaie eeneiou. Eco/aiea aiaeiae/iuo neiiao?e/iuo aeeaieeeaeia aeeeeiaeiiiauo eeneio iieacaei, /oi a oneiaeyo oa?iieeca iie ia?acotho niioaaonoaothuea aieeeaeu 3-aeeee-2,4-aeeienioeiieei-3-ea?aiiiauo eeneio, oiaaea eae a i?enoonoaee iniiaaiee oeeeeecaoeey oeacaiiuo aeeaieeeaeia nii?iaiaeaeaaony iouaieaieai ea?aaieeeaeiie a?oiie?iaee e i?eaiaeeo e ia?aciaaieth n aunieeie auoiaeaie 3-aeeee-4-aeae?iene-2-ienioeiieeiia. O/eouaay i?inoioo neioaca aeeaieeeaeia aeeeeiaeiiiauo eeneio, eioi?ua eaaei iiaeii iieo/eoue aoeeee?iaaieai aeeeeaio?aieeaoia aeeyoeeiauie yoe?aie eee aeeoei?aiaeae?eaeaie aeeeeiaeiiiauo eeneio, aeaiiue niinia ?aeiiaiaeiaai a ea/anoaa i?aia?aoeaiiai. ?aoeeiiaeueiia eniieueciaaiea aeeeeaio?aieeaoia i?e yoii aeinoeaaaony iooai iiaeai?a iaeaieaa iioeiaeueiiai niioiioaiey ?aaaaioia. Cia/eoaeueii ?anoe?yao aiciiaeiinoe iaoiaea eniieueciaaiea a ea/anoaa aoeeee?othueo aaaioia aeinooiiuo aeeoei?aiaeae?eaeia aeeeeiaeiiiauo eeneio, /oi iicaieyao eaaei neioace?iaaoue eae 1I-3-aeeee-4-aeae?iene-2-ienioeiieeiu, oae e eo 1-caiauaiiua aiaeiae. I?aaeeiaeaiiue niinia neioaca iaoae i?aeoe/aneia i?eiaiaiea ia oieueei aeey iieo/aiey 3-aeeee-, ii oaeaea e aeey neioaca ae?oaeo 3-caiauaiiuo 4-aeae?iene-2-ienioeiieeiia. Inouanoaeai neioac 4-I-aoeeeueiuo i?iecaiaeiuo 3-aeeee-4-aeae?iene-2-ienioeiieeiia iooai aoeeee?iaaiey iineaaeieo aiaeae?eaeaie eee oei?aiaeae?eaeaie ea?aiiiauo eeneio. Eco/aii iiaaaeaiea 3-aeeee-, 3-ea?aaeeiene-4-aeae?iene-2-ienioeiieeiia e 1-R-2,4-aeeieni-3I-oeiieei-3-ea?aiiiaeo eeneio a oneiaeyo a?iie?iaaiey iieaeoey?iui a?iiii. Onoaiiaeaii, /oi a?iie?iaaiea 1-R-2,4-aeeieni-3I-oeiieei-3-ea?aiiiauo eeneio ni?iaiaeaeaaony eo aeaea?aieneee?iaaieai, /oi aeaao aiciiaeiinoue ?aeiiaiaeiaaoue aeaiiue iaoiae a ea/anoaa i?aia?aoeaiiai aeey iieo/aiey 1-R-3-a?ii-4-aeae?iene-2-ienioeiieeiia. Oa?iieecii yoeeiauo yoe?ia 1-R-4-aeae?iene-2-ienioeiieei-3-ea?aiiiauo eeneio e 2-aieii-5-R-1,3,4-oeaaeeacieia iieo/aiu niioaaonaothuea aieaeu, iauaaeeiythuea a naiae no?oeoo?a aeaa oa?iaeioi?a. Anaai neioace?iaaii 71 ia iienaiiia a eeoa?aoo?a i?iecaiaeiia oeiieeia, no?oeoo?a e eiaeeaeaeoaeueiinoue eioi?uo iiaeoaa?aeaeaiu iaoiaeaie OO-, EE- e II?-niaeo?ineiiee, aeaiiuie yeaiaioiiai aiaeeca e oiieineieiie o?iiaoia?aoee, a ?yaea neo/aaa - ano?a/iui neioacii. I?iaaaeai aeieiae/aneee ne?eieia iieo/aiiuo aauanoa ia auyaeaiea aioeieneaeaioiie, iaia?aiinoaaeeece?othuae, aioeoe?aieaeiie, aeeo?aoe/aneie, i?ioeaiainiaeeoaeueiie, aioeiee?iaiie, aioeeiaaoeyioiie, aioe-AE*, i?ioeai?aeiaie, aa?aeoeeaeiie e ooiaeoeeaeiie aeoeaiinoe. Ii ?acoeueoaoai enneaaeiaaiey aeieiae/aneie aeoeaiinoe auyaeaiu yooaeoeaiua niaaeeiaiey iaia?aiinoaaeeece?othuaai, aioeieneaeaioiiai, aeeo?aoe/aneiai e aioeeiaaoeyioiiai aeaenoaey; onoaiiaeaiu ioaeaeueiua caeiiiia?iinoe nayce “no?oeoo?a aeaenoaea”. Iieacaia ia?niaeoeaa nicaeaiey ia iniiaa 5-R-1,3,4-oeaaeeacieee-2-aieaeia 1-R-4-aeae?iene-2-ienioeiieei-3-ea?aiiiauo eeneio iioaioeeaeueiuo ooiaeoeeaeia aeey ai?ueau n a?aaeeoaeyie naeueneioicyenoaaiiuo eoeueoo?. A ea/anoaa ia?niaeoeaiiai aaiaoii?ioaeoi?iiai n?aaenoaa i?aaeeiaeai 3-iiiee-4-aeae?iene-2-ienioeiieei, aeey eioi?iai ?ac?aaioai i?iaeo a?aiaiiie oa?iaeiiaeiie noaouee. Eeth/aaua neiaa: 4-aeae?iene-2-ienioeiieei, aeeeeaio?aieeaou, neioac, oa?iieec, aaoa?ioeeeeecaoeey, aaiaoii?ioaeoi?iia n?aaenoai. Evtifeeva O.A. The synthesis, physico-chemical and biological properties of 3-substituted-4-hydroxy-2-oxoquinolines. - Manuscript. The thesis for the Master Degree of Pharmacy in Speciality 15.00.02 - Pharmaceutical Chemistry and Pharmacognosy. - Ukrainian Academy of Pharmacy, Kharkov, 1999. New biologically active substances - 3-alkyl-4-hydroxy-2-oxoquinolines and their 4-O-acylderivatives; 3-bromosubstituted-2,4-dioxoquinolines; 5-R-1,3,4-thidiazolyl-2-amides 1-R-4-hydroxy-2-oxoquinolines of 3-carboxylic acids - have been studied in the range of 3-substituted hydroxy(oxo)quinolines. The synthetic preparative methods for 3-alkyl-4-hydroxy-2-oxoquinolines and 1-R-3-brom-4-hydroxy-2-oxoquinolines have been developed. For the first time the possibility of the Dickman condensation realization was shown under thermolysis conditions. Unlike the classic conditions it is carried out in the absence of the basic catalysts. So the possible mechanism of this transformation has been suggested. UV-, IR-, PMR-spectra characteristics of the compounds synthesized have been studied. During the pharmacological screening effective substances with membranostabilizing, antioxidant, diuretic, anticoagulant and fungicidic activities have been revealed and some regularities of the “structure-action” relation have been established. The most perspective compound has been recommended as a potential hepatoprotective agent. Key words: 4-hydroxy-2-oxoquinoline, alkylanthranilates, synthesis, thermolysis, heterocyclisation, hepatoprotective agent.

Нашли опечатку? Выделите и нажмите CTRL+Enter

Похожие документы
Обсуждение

Оставить комментарий

avatar
  Подписаться  
Уведомление о
Заказать реферат!
UkrReferat.com. Всі права захищені. 2000-2020