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ID: ALA1138940
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Authors: Wu WL, Burnett DA, Caplen MA, Domalski MS, Bennett C, Greenlee WJ, Hawes BE, O'Neill K, Weig B, Weston D, Spar B, Kowalski T.
Abstract: Biaryl urea lead compound 1 was discovered earlier in our MCH antagonist program. Novel benzimidazole analogues with increased chemical stability, devoid of the potential carcinogenic liability associated with a biarylamine moiety, were synthesized and evaluated to be potent MCH R1 antagonists. Two compounds in this series have demonstrated in vivo efficacy in a rodent obesity model.
CiteXplore: 16690315