HIV PROTEASE INHIBITORY BIS-BENZAMIDE CYCLIC UREAS - A QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSIS

A series of N,N'-disubstituted cyclic urea 3-benzamides has been synth esized and evaluated for HIV protease inhibition and antiviral activit y. Some of these benzamides have been shown to be potent inhibitors of HIV protease with K-i < 0.050 nM and IC90 < 20 nM for viral replicati on and, as such, may be useful in the treatment of AIDS. The synthesis and quantitative structure-activity relationship for this benzamide s eries will be discussed.