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ID: ALA1833830
Journal: Bioorg Med Chem
Title: 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
Authors: Novikov MS, Ivanova ON, Ivanov AV, Ozerov AA, Valuev-Elliston VT, Temburnikar K, Gurskaya GV, Kochetkov SN, Pannecouque C, Balzarini J, Seley-Radtke KL.
Abstract: 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 ω-(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.
CiteXplore: 21903401