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1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors ofTrypanosoma cruzi in mice
Authors:J C Chabala  V B Waits  T Ikeler  A A Patchett  L Payne  L H Peterson  R A Reamer  K Hoogsteen  M Wyvratt  W L Hanson  M H Fisher
Institution:(1) Merck Sharp & Dohme Research Laboratories, 07065 Rahway, New Jersey, USA;(2) College of Veterinary Medicine, University of Georgia, 30602 Athens, Georgia, USA
Abstract:Summary 1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors ofTrypanosoma cruzi infections in mice. The most active compounds are the 1-(4-chlorobenzyl)- and 1-(3,4-dichlorobenzyl)-analogs (L-153,094 2] and L-153,153 4], resp.) which are approximately 7-fold more potent upon oral administration than nifurtimox (Lampit) in suppressing parasite levels in the blood of mice with acuteTrypanosoma cruzi infections.
Keywords:1-(Substituted)-benzyl-5-aminoimidazole-4-carboxamide  T  cruzi  Chagas' disease
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