antibioticsАнтибиотики и ХимиотерапияAntibiot Khimioter = Antibiotics and Chemotherapy0235-2990ООО «Издательство ОКИ»antibiotics-23Research ArticleОРИГИНАЛЬНЫЕ СТАТЬИORIGINAL PAPERSНовые биологически активные соединения в ряду производных 3-(индол-1-ил)-, З-(N-аминоарил)- и 3-(S-тиоарил)малеимидаNew Biologically Active Compounds in the Series of 3-(indol-1-yl)-, 3-(N-aminoaryl)-, and 3-(S-thioaryl)Maleimide DerivativesЛакатошС. А.LakatoshS. A.lakatosh@inbox.ruТренинА. С.TreninA. S'.noemail@neicon.ruСимоновА. Ю.SimonovA. Yu.noemail@neicon.ruЛавреновС. Н.LavrenovS. N.noemail@neicon.ruБычковаО. П.BychkovaO. P.noemail@neicon.ruЦвигунЕ. А.TsvigunE. A.noemail@neicon.ruФГБНУ «НИИ по изысканию новых антибиотиков имени Г.Ф.Гаузе»РоссияGause Institute of New AntibioticsRussian FederationНИИ по изысканию новых антибиотиков им. Г. Ф. ГаузеРоссияGause Institute of New AntibioticsRussian Federation201706052020625-6311Copyright © Лакатош С.А., Тренин А.С., Симонов А.Ю., Лавренов С.Н., Бычкова О.П., Цвигун Е.А., 20202020Лакатош С.А., Тренин А.С., Симонов А.Ю., Лавренов С.Н., Бычкова О.П., Цвигун Е.А.Lakatosh S.A., Trenin A.S., Simonov A.Y., Lavrenov S.N., Bychkova O.P., Tsvigun E.A.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.antibiotics-chemotherapy.ru/jour/article/view/23

Путём полного химического синтеза получены новые соединения в ряду 3,4-дизамещённых производных малеимвда, обладающие выраженной антимикробной активностью in vitro в отношении грамположигельных бактерий, дрожжей Candida albicans и грибов Aspergillus niger. Одновременно все изученные соединения оказались неактивными в отношении грамотрицательных бактерий Escherichia coli, что свидетельствует о специфическом характере их антимикробного действия. Ряд производных проявили себя в тест-системе с бактериальной культурой Halobacterium salinarum, используемой для отбора биологически активных соединений - ингибиторов биосинтеза стеролов и противоопухолевых антибиотиков, что позволяет предполагать наличие у них потенциальных противоопухолевых свойств. Наибольшую биологическую активность проявили З-бромо-4-тиоарильные и 3,4-бистиоарильное производные, относящиеся к новому типу химических соединений, перспективных для дальнейшего изучения и создания на их основе новых антимикробных и противоопухолевых лекарственных средств.

Novel compounds among 3,4-disubstituted maleimlde derivatives that reveal a pronounced antimicrobial activity in vitro against Gram-positive bacteria, yeast Candida albicans, and fungi Aspergillus niger were obtained through total chemical synthesis. All these derivatives were simultaneously inactive against Gram-negative bacteria Escherichia coli, indicating the specific nature of their antimicrobial action. A number of derivatives appeared to be active in Halobacterium salinarum test system, which is used for selecting biologically active compounds among sterol biosynthesis inhibitors and antitumor antibiotics. This data suggests that such derivatives seem to have potential antitumor properties. The most active compounds were 3-bromo-4-thioaryl and 3,4-bisthioaryl maleimides, which are related to a new type of chemical compounds, that are promising for further elaboration and development of new antimicrobial and antitumordrugs on their basis.

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The authors declare that there are no conflicts of interest present.