Article
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
Bioorganic & medicinal chemistry letters - 15 Feb 2006
Smith Amos B, Charnley Adam K, Harada Hironori, Beiger Jason J, Cantin Louis-David, Kenesky Craig S, Hirschmann Ralph, Munshi Sanjeev, Olsen David B, Stahlhut Mark W, Schleif William A, Kuo Lawrence C
Abstract excerpt
A series of monopyrrolinone-based HIV-1 protease inhibitors possessing rationally designed P2' side chains have been synthesized and evaluated for activity against wild-type HIV-1 protease. The most potent inhibitor displays subnanomolar potency in vitro for the wild-type HIV-1 protease. Additionally, the monopyrrolinone inhibitors retain potency in cellular assays against clinically significant mutant forms of...
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