title: Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
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.
authors.affiliation: Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA. wen-lian.wu@spcorp.com
authors.forename: Wen-Lian
authors.initials: WL
authors.lastname: Wu
authors.forename: Duane A
authors.initials: DA
authors.lastname: Burnett
authors.forename: Mary Ann
authors.initials: MA
authors.lastname: Caplen
authors.forename: Martin S
authors.initials: MS
authors.lastname: Domalski
authors.forename: Chad
authors.initials: C
authors.lastname: Bennett
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Brian E
authors.initials: BE
authors.lastname: Hawes
authors.forename: Kim
authors.initials: K
authors.lastname: O'Neill
authors.forename: Blair
authors.initials: B
authors.lastname: Weig
authors.forename: Daniel
authors.initials: D
authors.lastname: Weston
authors.forename: Brian
authors.initials: B
authors.lastname: Spar
authors.forename: Timothy
authors.initials: T
authors.lastname: Kowalski
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects*; D004195:Disease Models, Animal; D015195:Drug Design; D051381:Rats; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D019440:Anti-Obesity Agents; D001562:Benzimidazoles; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor