Novel 3-Nitro-1H-1,2,4-triazole-Based Amides and Sulfonamides as Potential Antitrypanosomal Agents

Abstract

A series of novel 3-nitro-1H-1,2,4-triazole-based (and in some cases 2-nitro-1H-imidazole-based) amides and sulfonamides were characterized for their in vitro antitrypanosomal and antileishmanial activities as well as mammalian toxicity. Out of 36 compounds tested, 29 (mostly 3-nitro-1H-1,2,4-triazoles) displayed significant activity against Trypanosoma cruzi intracellular amastigotes (IC50 ranging from 28 nM to 3.72 μM) without concomitant toxicity to L6 host cells (selectivity 66–2782). Twenty-three of these active compounds were more potent (up to 58-fold) than the reference drug benznidazole, tested in parallel. In addition, nine nitrotriazoles which were moderately active (0.5 μM ≤ IC50

Citation

Papadopoulou, M.V.; Bloomer, W.D.; Rosenzweig, H.S.; Chatelain, E.; Kaiser, M.; Wilkinson, S.R.; McKenzie, C.; Ioset, J.R. Novel 3-Nitro-1H-1,2,4-triazole-Based Amides and Sulfonamides as Potential Antitrypanosomal Agents. Journal of Medicinal Chemistry (2012) 55 (11) 5554-5565. [DOI: 10.1021/jm300508n]

Novel 3-Nitro-1H-1,2,4-triazole-Based Amides and Sulfonamides as Potential Antitrypanosomal Agents

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