Synthesis of Pyrryl Aryl Sulfones Targeted at the HIV-1 Reverse Transcriptase
Autor: | Marino Artico, Romano Silvestri, Giorgio Stefancich, E. Pagnozzi, P. La Colla, D. Musu, E. Tinti, Silvio Massa, Elisabetta Pinna, F. Scintu |
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Rok vydání: | 1995 |
Předmět: |
chemistry.chemical_classification
biology Cell Survival Stereochemistry Aryl Pharmaceutical Science Chemical synthesis HIV Reverse Transcriptase Sulfone Sulfonamide Structure-Activity Relationship chemistry.chemical_compound chemistry Enzyme inhibitor HIV-2 Drug Discovery HIV-1 biology.protein Humans Reverse Transcriptase Inhibitors Structure–activity relationship Pyrroles Sulfones Cytotoxicity Lead compound |
Zdroj: | Archiv der Pharmazie. 328:223-229 |
ISSN: | 1521-4184 0365-6233 |
DOI: | 10.1002/ardp.19953280304 |
Popis: | 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). |
Databáze: | OpenAIRE |
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