CYCLIC SULFONE-3-CARBOXAMIDES AS NOVEL P(2)-LIGANDS FOR Ro 31-8959 BASED HIV-1 PROTEASE INHIBITORS

Cyclic sulfone-3-carboxamides are effective P(2)-1igands for HIV-1 protease inhibitors. Incorporation of 3S-tetrahydro-2H-thiopyrancarboxamide-l, l-dioxide in the hydroxyethylamine series resulted in inhibitor 14 (IC(50)=9 nM, CIC(95)=200 nM) with improved potency compared to its corresponding urethane derivative 18 (IC(50)=2.0 μM).