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Synthesis and biological evaluation of aryl-phospho-indole as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. 2011
François-René Alexandre, and
Agnès Amador, and
Stéphanie Bot, and
Catherine Caillet, and
Thierry Convard, and
Jocelyn Jakubik, and
Chiara Musiu, and
Barbara Poddesu, and
Luana Vargiu, and
Michel Liuzzi, and
Arlène Roland, and
Maria Seifer, and
David Standring, and
Richard Storer, and
Cyril B Dousson
Laboratoires Idenix, Département de Chimie Médicinale, Montpellier, France. alexandre.francois-rene@idenix.com
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 enantiomers showed that only R enantiomer retained the activity. The pharmacokinetic, solubility, and metabolic properties of 14 were assessed.
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