1-Arylsulfonyl-3-(Alpha-Hydroxybenzyl)-1h-Pyrroles, A Novel Class Of Anti-Hiv-1 Reverse Transcriptase Inhibitors

Various 1-arylsulfonyl-3-(alpha-hydroxybenzyl)-1H-pyrroles were prepared by Friedel-Crafts reaction of 1-aryisulfonyl-1H-pyrroles with aroylchlorides in the presence of aluminum trichloride, followed by reduction of the ketones to the required carbinols. Title compounds were identified as a novel class of nonnucleoside HIV-1 reverse transcriptase inhibitors characterized by the presence of a diarylcarbinol moiety, a chemical feature that strictly correlates with the anti-HTV-1 activity. (C) 1997 Elsevier Science Ltd.