CYCLIC SULFONE-3-CARBOXAMIDES AS NOVEL P2-LIGANDS FOR Ro 31-8959 BASED HIV-1 PROTEASE INHIBITORS

Bioorg Med Chem Lett. 1995 Jan 5;5(1):83-88. doi: 10.1016/0960-894X(94)00463-P. Epub 2000 Mar 29.

Abstract

Cyclic sulfone-3-carboxamides are effective P2-1igands for HIV-1 protease inhibitors. Incorporation of 3S-tetrahydro-2H-thiopyrancarboxamide-l, l-dioxide in the hydroxyethylamine series resulted in inhibitor 14 (IC50=9 nM, CIC95=200 nM) with improved potency compared to its corresponding urethane derivative 18 (IC50=2.0 μM).