1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents
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Novikov, Mikhail S., Olga N. Ivanova, Alexander V. Ivanov, Alexander A. Ozerov, Vladimir T. Valuev-Elliston, Kartik Temburnikar, Galina V. Gurskaya, et al. “1-[2-(2-Benzoyl- and 2-Benzylphenoxy)Ethyl]Uracils as Potent Anti-HIV-1 Agents.” Bioorganic & Medicinal Chemistry 19, no. 19 (October 1, 2011): 5794–5802. https://doi.org/10.1016/j.bmc.2011.08.025.
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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.