The Synthesis and Evaluation of Cyclic Ureas as HIV Protease Inhibitors: Modifications of the P1/P1′ Residues.

Abstract Two series of cyclic ureas modified at the P1/P1′ residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-methoxy analog) showed significant improvement in antiviral activity relative to lead compounds DMP323 and DMP 450.