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Synthesis, evaluation of C-5 modified 2 '-deoxyuridine monophosphates as inhibitors of M-tuberculosis thymidylate synthaseстатья
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 11 января 2016 г.
- Авторы: Alexandrova Liudmila A., Chekhov Vladimir O., Shmalenyuk Eduard R., Kochetkov Sergey N., Abu El-Asrar Rania, Herdewijn Piet
- Журнал: Bioorganic and Medicinal Chemistry
- Том: 23
- Номер: 22
- Год издания: 2015
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- Первая страница: 7131
- Последняя страница: 7137
- Аннотация: A series of 5'-monophosphates of 5-substituted 2'-deoxyuridine analogs, which recently demonstrated in vitro substantial suppression of two strains of Mycobacterium tuberculosis growth (virulent laboratory H37Rv and multiple resistant MS-115), has been synthesized and evaluated as potential inhibitors of M. tuberculosis thymidylate synthases: classical (ThyA) and flavin dependent thymidylate synthase (ThyX). A systematic SAR study and docking revealed 5-undecyloxymethyl-2'-deoxyuridine 5'-monophosphate 3b, displaying an IC50 value against ThyX of 8.32 mu M. All derivatives lack activity against the ThyA. It can be assumed that the mechanism of action of 3b may be partially associated with the inhibition of the ThyX. (C) 2015 Elsevier Ltd. All rights reserved.
- Добавил в систему: Кочетков Сергей Николаевич