title: 1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice.
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.
authors.affiliation: Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
authors.forename: J C
authors.initials: JC
authors.lastname: Chabala
authors.forename: V B
authors.initials: VB
authors.lastname: Waits
authors.forename: T
authors.initials: T
authors.lastname: Ikeler
authors.forename: A A
authors.initials: AA
authors.lastname: Patchett
authors.forename: L
authors.initials: L
authors.lastname: Payne
authors.forename: L H
authors.initials: LH
authors.lastname: Peterson
authors.forename: R A
authors.initials: RA
authors.lastname: Reamer
authors.forename: K
authors.initials: K
authors.lastname: Hoogsteen
authors.forename: M
authors.initials: M
authors.lastname: Wyvratt
authors.forename: W L
authors.initials: WL
authors.lastname: Hanson
mesh_terms: D000620:Aminoimidazole Carboxamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D014355:Chagas Disease / Q000188:drug therapy*; D003198:Computer Simulation; D005260:Female; D051379:Mice; D008815:Mice, Inbred Strains; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014349:Trypanosoma cruzi
chemical_list: D000981:Antiprotozoal Agents; D000620:Aminoimidazole Carboxamide