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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

DOI: 10.1016/j.bmcl.2006.04.062