1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors ofTrypanosoma cruzi in mice |
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| 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 |
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| Affiliation: | (1) Merck Sharp & Dohme Research Laboratories, 07065 Rahway, New Jersey, USA;(2) College of Veterinary Medicine, University of Georgia, 30602 Athens, Georgia, USA |
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| 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. |
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| Keywords: | 1-(Substituted)-benzyl-5-aminoimidazole-4-carboxamide T. cruzi Chagas' disease |
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