Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand.

1998 
Abstract A series of novel unsymmetrical anthranilamide-containing HIV protease inhibitors was designed. The structure-activity studies revealed a series of potent P2–P3′ inhibitors that incorporate an anthranilamide group at the P2′ position. A reduction in molecular weight and lipophilicity is achieved by a judicious choice of P2 ligands (i.e., aromatic, heteroaromatic, carbamate, and peptidic). A systematic investigation led to the 5-thiazolyl carbamate analog 8m , which exhibited a favorable C max EC 50 ratio (>30), plasma half-life (>8 h), and potent in vitro antiviral activity (EC 50 = 0.2 uM).
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