Sainte-Foy-lès-Lyon, France
Sainte-Foy-lès-Lyon, France

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Alexandre F.-R.,Laboratoires Idenix | Amador A.,Laboratoires Idenix | Bot S.,Laboratoires Idenix | Caillet C.,Laboratoires Idenix | And 11 more authors.
Journal of Medicinal Chemistry | Year: 2011

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. © 2010 American Chemical Society.


PubMed | Laboratoires Idenix
Type: Journal Article | Journal: Journal of medicinal chemistry | Year: 2011

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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