M. Artico et al., -ARYLSULFONYL-3-(ALPHA-HYDROXYBENZYL)-1H-PYRROLES, A NOVEL CLASS OF ANTI-HIV-1 REVERSE-TRANSCRIPTASE INHIBITORS, Bioorganic & medicinal chemistry letters, 7(14), 1997, pp. 1931-1936
Various 1-arylsulfonyl-3-(alpha-hydroxybenzyl)-1H-pyrroles were prepar
ed by Friedel-Crafts reaction of 1-aryisulfonyl-1H-pyrroles with aroyl
chlorides in the presence of aluminum trichloride, followed by reducti
on of the ketones to the required carbinols. Title compounds were iden
tified as a novel class of nonnucleoside HIV-1 reverse transcriptase i
nhibitors 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.