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Synthesis of Pyrryl Aryl Sulfones Targeted at the HIV‐1 Reverse Transcriptase
Author(s) -
Artico Marino,
Silvestri Romano,
Stefancich Giorgio,
Massa Silvio,
Pagnozzi Eugenia,
Musu Daniela,
Scintu Franca,
Pinna Elisabetta,
Tinti Enrico,
La Colla Paolo
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280304
Subject(s) - sulfone , aryl , chemistry , human immunodeficiency virus (hiv) , reverse transcriptase , in vitro , cytotoxicity , stereochemistry , chemical synthesis , combinatorial chemistry , organic chemistry , biochemistry , medicine , virology , rna , alkyl , gene
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).