Article
Synthesis and biological evaluation of aryl-phospho-indole as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry - 13 Jan 2011
Alexandre François-René, Amador Agnès, Bot Stéphanie, Caillet Catherine, Convard Thierry, Jakubik Jocelyn, Musiu Chiara, Poddesu Barbara, Vargiu Luana, Liuzzi Michel, Roland Arlène, Seifer Maria, Standring David, Storer Richard, Dousson Cyril B
Abstract excerpt
A novel series of 3-aryl-phospho-indole (API) non-nucleoside reverse transcriptase inhibitors of HIV-1 was developed. Chemical variation in the phosphorus linker led to the discovery of 3-phenyl-methyl-phosphinate-2-carboxamide 14, which possessed excellent potency against wild-type HIV-1 as well as viruses bearing K103N and Y181C single mutants in the reverse transcriptase gene. Chiral separation of the...
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