1053741-29-9Relevant academic research and scientific papers
Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2' groups
Rodgers, James D.,Johnson, Barry L.,Wang, Haisheng,Greenberg, Roger A.,Erickson-Viitanen, Susan,Klabe, Ronald M.,Cordova, Beverly C.,Rayner, Marlene M.,Lam, Gilbert N.,Chang, Chong-Hwan
, p. 2919 - 2924 (2007/10/03)
A series of benzofused heterocycles was examined to replace the metabolically unstable benzyl alcohol P2/P2' groups of DMP 323 (1). Extremely potent inhibitors of HIV protease (Ki 90 = 8 nM) were found. An X-ray crystal structure of benzimidazolone 5a bound to HIV protease showed H-bonds to Asp30 and a bridging water molecule to Gly48.
