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

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3674-3678
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antagonist Anti-Obesity Agents - chemical synthesis Anti-Obesity Agents - pharmacology Benzimidazoles - chemical synthesis Benzimidazoles - pharmacology Biological and medical sciences Body Weight - drug effects Disease Models, Animal Drug Design Hormones. Endocrine system Medical sciences Melanin-concentrating hormone receptor Obesity Pharmacology. Drug treatments Rats Receptors, Pituitary Hormone - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.04.062