RU2012122441A - METHOD FOR MODIFICATION OF THE MACROLIDE ANTIBIOTIC OF OLIGOMYCIN A USING THE REACTION OF [3 + 2] -DIPOLAR CYCLE CONNECTION OF ASIDE AND ALKINES, 33-DESOKIS-33- (TRIAZOL-1-ILIOROCHILOISOLEBILI - Google Patents

METHOD FOR MODIFICATION OF THE MACROLIDE ANTIBIOTIC OF OLIGOMYCIN A USING THE REACTION OF [3 + 2] -DIPOLAR CYCLE CONNECTION OF ASIDE AND ALKINES, 33-DESOKIS-33- (TRIAZOL-1-ILIOROCHILOISOLEBILI Download PDF

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RU2012122441A
RU2012122441A RU2012122441/04A RU2012122441A RU2012122441A RU 2012122441 A RU2012122441 A RU 2012122441A RU 2012122441/04 A RU2012122441/04 A RU 2012122441/04A RU 2012122441 A RU2012122441 A RU 2012122441A RU 2012122441 A RU2012122441 A RU 2012122441A
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oligomycin
triazol
dipolar
iliorochiloisolebili
desokis
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RU2012122441/04A
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RU2523284C9 (en
RU2523284C2 (en
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Ольга Борисовна Беккер
Валерий Николаевич Даниленко
Людмила Николаевна Лысенко
Алексей Михайлович Королев
Елена Николаевна Бычкова
Любовь Георгиевна Деженкова
Александр Альбертович Штиль
Мария Николаевна ПРЕОБРАЖЕНСКАЯ
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Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан"
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Abstract

1. Способ получения производных антибиотика олигомицина А, заключающийся в региоселективном [3+2]-диполярном циклоприсоединении азидогруппы 33-дезокси-33-азидоолигомицина А(1) к монозамещенным алкинам 2а-в (Схема 2).2. Производные антибиотика олигомицина А 3а-г, соответствующие общей формуле:где R представляет собой 1,4-дизамещенные 1,2,3-триазолы: а. - (фенил-триазол-1-ил), б. -(4-карбокси-триазол-1-ил), в. -(4-4-метоксикарбонил-триазол-1-ил), г. -(4-диметиламиноэтиламидокарбокситриазол-1-ил).3. Применение соединений формулы 3а-г из п.1 в качестве биологически активных веществ, перспективных для создания противоопухолевых лекарств.1. A method for producing derivatives of the antibiotic oligomycin A, which consists in the regioselective [3 + 2] -dipolar cycloaddition of the azido group of 33-deoxy-33-azido-oligomycin A (1) to monosubstituted alkynes 2a-b (Scheme 2) .2. Derivatives of the antibiotic oligomycin A 3a-g, corresponding to the general formula: where R is 1,4-disubstituted 1,2,3-triazoles: a. - (phenyl-triazol-1-yl), b. - (4-carboxy-triazol-1-yl), c. - (4-4-methoxycarbonyl-triazol-1-yl), g. - (4-dimethylaminoethylamidocarboxytriazol-1-yl). 3. The use of compounds of formula 3a-g of claim 1 as biologically active substances promising for the creation of antitumor drugs.

Claims (3)

1. Способ получения производных антибиотика олигомицина А, заключающийся в региоселективном [3+2]-диполярном циклоприсоединении азидогруппы 33-дезокси-33-азидоолигомицина А(1) к монозамещенным алкинам 2а-в (Схема 2).1. The method of producing derivatives of the antibiotic oligomycin A, which consists in regioselective [3 + 2] -dipolar cycloaddition of the azido group of 33-deoxy-33-azido-oligomycin A (1) to monosubstituted alkynes 2a-b (Scheme 2). 2. Производные антибиотика олигомицина А 3а-г, соответствующие общей формуле:2. Derivatives of the antibiotic oligomycin A 3a-g, corresponding to the General formula:
Figure 00000001
Figure 00000001
 где R представляет собой 1,4-дизамещенные 1,2,3-триазолы: а. - (фенил-триазол-1-ил), б. -(4-карбокси-триазол-1-ил), в. -(4-4-метоксикарбонил-триазол-1-ил), г. -(4-диметиламиноэтиламидокарбокситриазол-1-ил).where R represents a 1,4-disubstituted 1,2,3-triazole: a. - (phenyl-triazol-1-yl), b. - (4-carboxy-triazol-1-yl), c. - (4-4-methoxycarbonyl-triazol-1-yl), g. - (4-dimethylaminoethylamidocarboxytriazol-1-yl). 3. Применение соединений формулы 3а-г из п.1 в качестве биологически активных веществ, перспективных для создания противоопухолевых лекарств. 3. The use of compounds of formula 3a-g of claim 1 as biologically active substances promising for the creation of antitumor drugs.
RU2012122441/04A 2012-05-31 2012-05-31 Method for modification of macrolide antibiotic oligomycin a by reaction of [3+2]-dipolar cycloconnection of azide and alkines 33-deoxy-33-(triazol-1-yl)-oligomycins a and their biological activity RU2523284C9 (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2623087C1 (en) * 2016-11-03 2017-06-22 Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт по изысканию новых антибиотиков имени Г.Ф. Гаузе" Method for 2,3,16,17,18,19-hexahydrooligomycin a and its application for inhibiting growth of candida yeasts

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SK284041B6 (en) * 1996-08-28 2004-08-03 The Procter And Gamble Company Spirocyclic metalloprotease inhibitors
WO2012028556A1 (en) * 2010-08-31 2012-03-08 Bayer Animal Health Gmbh Macrocyclic lactones and their use and their combinations with other active substances

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2623087C1 (en) * 2016-11-03 2017-06-22 Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт по изысканию новых антибиотиков имени Г.Ф. Гаузе" Method for 2,3,16,17,18,19-hexahydrooligomycin a and its application for inhibiting growth of candida yeasts

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