Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors

Imidazolidinones were synthesized from 7-membered ring cyclic ureas via a sequential series of novel ring contraction reactions proceeding first through the tetrahydropyrimidinones and finally to the 5-membered ring heterocycle. These imidazolidinones are shown to be excellent HIV-PR inhibitors. The most potent compound 20 having a Ki = 17 nM.