National Center for
2FDD: Crystal Structure Of Hiv Protease D545701 Bound With Gw0385
Bioorg. Med. Chem. Lett. (2006) 16 p.1788-1794
A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.