Archiv der Pharmazie (Weinheim) 1995-03-01

Synthesis of pyrryl aryl sulfones targeted at the HIV-1 reverse transcriptase.

M Artico, R Silvestri, G Stefancich, S Massa, E Pagnozzi, D Musu, F Scintu, E Pinna, E Tinti, P La Colla

Index: Arch. Pharm. (Weinheim) 328(3) , 223-9, (1995)

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Abstract

Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1. 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Some structure-activity relationships are discussed also in comparison with the known NPPS (2-nitrophenyl phenyl sulfone).