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. Source