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1 Polish Journal of Chemistry

1 2006

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Synthesis of N,S-Substituted 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives as Potential Anti-HIV Agents

Brzozowski Z., Sławiński J.

Polish Journal of Chemistry

2006

Vol. 80, nr 11

1807-1815

A new series of N,S-substituted 4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives 12-15, 17, 18 and 20-24 have been synthesized as potential anti-HIV agents. All compounds were screened at the National Cancer Institute (Bethesda, USA) for their in vitro anti-HIV-1 activity, and relationships between structure and anti-HIVactivity are discussed. The prominent compounds with remarkable activity were [5-chloro- 4-methyl-2-(1H-pyrrol-1-ylsulfonyl)phenylthio]acetamide 22 (EC50 = 5.9 _M) and 4-bromophenyl 5-chloro-4-methyl-2-(1H-pyrrol-1-ylsulfonyl)phenylthiomethyl ketone 4-phenylsemicarbazone 24 (EC50 = 5.1 mi M).