Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists

…, BE Hawes, K O'Neill, B Weig, D Weston, B Spar…

Index: Wu, Wen-Lian; Burnett, Duane A.; Caplen, Mary Ann; Domalski, Martin S.; Bennett, Chad; Greenlee, William J.; Hawes, Brian E.; O'Neill, Kim; Weig, Blair; Weston, Daniel; Spar, Brian; Kowalski, Timothy Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 14 p. 3674 - 3678

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Citation Number: 17

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.