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1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma 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
Affiliation:Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
Abstract:1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma 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 acute Trypanosoma cruzi infections.
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