1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents
2011
Novikov, Mikhail S. | Ivanova, Olga N. | Ivanov, A. V. | Ozerov, Alexander A. | Valuev-Elliston, Vladimir T. | Temburnikar, Kartik | Gurskai︠a︡, G. V. (Galina Viktorovna) | Kochetkov, Sergey N. | Pannecouque, Christophe | Balzarini, Jan | Seley-Radtke, Katherine L.
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.
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