898128-51-3Relevant articles and documents
CATECHOL DIETHERS AS POTENT ANTI-HIV AGENTS
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Page/Page column 49-50, (2013/04/25)
The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or sec
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyluracils as potent anti-HIV-1 agents
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,Seley-Radtke, Katherine L.
experimental part, p. 5794 - 5802 (2011/11/04)
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.
