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Synthesis of Pyrryl Aryl Sulfones Targeted at the HIV-1 Reverse Transcriptase

✍ Scribed by Marino Artico; Romano Silvestri; Giorgio Stefancich; Silvio Massa; Eugenia Pagnozzi; Daniela Musu; Franca Scintu; Elisabetta Pinna; Enrico Tinti; Paolo La Colla

Publisher: John Wiley and Sons
Year: 1995
Tongue: English
Weight: 581 KB
Volume: 328
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19953280304

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✦ Synopsis

Various aryl I-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1. 2-Nitrophenyl-2-ethoxycarbonyl-1 -pynyl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitru 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).

Synthese von Pyrryl-aryl-sulfonen als Hemmstoffe der Reversen Transkriptase des HIV-1

Verschiedene l-Pyrryl-sulfone werden synthetisiert und auf Hemmwirkung gegen HIV-1 gepriift. 2-Nitrophenyl-2-ethoxycarbonyl-l-pynyl-sulfon, die wirksarnste der Test-Verbindungen, wurde zur Leitsubstanz in der Aryl-pyrryl-sulfon-Reihe.

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