Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation

by Papadopoulou MV, Bloomer WD, Rosenzweig HS, O’Shea IP, Wilkinson SR, Kaiser M, Chatelain E, Ioset JR. Bioorganic Medicinal Chemistry. 2015 Aug 24. pii: S0968-0896(15)00681-1. doi: 10.1016/j.bmc.2015.08.014.

Summary: The manuscript describes the synthesis and evaluation of several nitroimidazole amides as antitrypanosomal agents. Compounds were potent and selective to differing degrees against parasitic forms of Trypanosoma cruzi and Leishmania donovanii, although no compound showed activity against T.brucei rhodesienese. The most potent in vitro anti-T. cruzi compounds constitute a new generation of effective and more affordable antitrypanosomal agents.

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