Reaction of benzenesulfonyl chlorides with 1H-pyrrole afforded the related 1-benzenesulfonyl pyrroles, which were transformed into the corresponding 3-aroyl derivatives by Friedel-Crafts condensation. Reduction of the ketone group led to 1-arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles. When assayed on MT-4 cells some carbinol derivatives were found to be active against HIV-1 at low micromolar concentrations.

1-Arylsulfonyl-3-(a-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors / Artico, M.; DI SANTO, Roberto; Costi, Roberta; Massa, S.; Scintu, F.; Loi, A. G.; DE MONTIS, A.; LA COLLA, P.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 7:14(1997), pp. 1931-1936. [10.1016/S0960-894X(97)00340-5]

1-Arylsulfonyl-3-(a-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors.

DI SANTO, Roberto;COSTI, Roberta;
1997

Abstract

Reaction of benzenesulfonyl chlorides with 1H-pyrrole afforded the related 1-benzenesulfonyl pyrroles, which were transformed into the corresponding 3-aroyl derivatives by Friedel-Crafts condensation. Reduction of the ketone group led to 1-arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles. When assayed on MT-4 cells some carbinol derivatives were found to be active against HIV-1 at low micromolar concentrations.
1997
HIV/AIDS; HIV NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
01 Pubblicazione su rivista::01a Articolo in rivista
1-Arylsulfonyl-3-(a-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors / Artico, M.; DI SANTO, Roberto; Costi, Roberta; Massa, S.; Scintu, F.; Loi, A. G.; DE MONTIS, A.; LA COLLA, P.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 7:14(1997), pp. 1931-1936. [10.1016/S0960-894X(97)00340-5]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/245262
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