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1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agentsстатья
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 декабря 2015 г.
- Авторы: Novikov Mikhail S., Ivanova Olga N., Ivanov Alexander V., Ozerov Alexander A., Valuev-Elliston Vladimir T., Temburnikar Kartik, Gurskaya Galina V., Kochetkov Sergey N., Pannecouque Christophe, Balzarini Jan
- Журнал: Bioorganic and Medicinal Chemistry
- Том: 19
- Номер: 19
- Год издания: 2011
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- Первая страница: 5794
- Последняя страница: 5802
- DOI: 10.1016/j.bmc.2011.08.025
- Аннотация: Non-nucleoside reverse transcriptase inhibitors (NNRTI) are key components in highly active antiretroviral therapy for treating HIV-1. Herein we present the synthesis for a series of N1-alkylated uracil derivatives bearing omega-(2-benzyl- and 2-benzoylphenoxy)alkyl substituents as novel NNRTIs. These compounds displayed anti-HIV activity similar to that of nevirapine and several of them exhibited activity against the K103N/Y181C RT mutant HIV-1 strain. Further evaluation revealed that the inhibitors were active against most nevirapine-resistant mono- and di-substituted RTs with the exception of the V106A RT. Thus, the candidate compounds can be regarded as potential lead compounds against the wild-type virus and drug-resistant forms.
- Добавил в систему: Кочетков Сергей Николаевич