title: Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists.
abstract: The synthesis and biological evaluation of novel pyrazole and imidazole carboxamides as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced on rimonabant template. The central pyrazole core was also replaced with its conformationally constrained motif and imidazole moieties. In general, a range of modifications were well tolerated. Several molecules with low- and sub-nanomolar potencies were identified as potent CB1 receptor antagonists. The in vivo proof of principle for weight loss is demonstrated with a lead compound in DIO mice model.
authors: Discovery Research, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500049, India. sasmalpk@yahoo.co.in
authors: Pradip K
authors: PK
authors: Sasmal
authors: Rashmi
authors: R
authors: Talwar
authors: J
authors: J
authors: Swetha
authors: D
authors: D
authors: Balasubrahmanyam
authors: B
authors: B
authors: Venkatesham
authors: Khaji Abdul
authors: KA
authors: Rawoof
authors: B
authors: B
authors: Neelima Devi
authors: Vikram P
authors: VP
authors: Jadhav
authors: Sanjoy K
authors: SK
authors: Khan
authors: Priya
authors: P
authors: Mohan
authors: D
authors: D
authors: Srinivasa Reddy
authors: Vijay Kumar
authors: VK
authors: Nyavanandi
authors: Srinivas
authors: S
authors: Nanduri
authors: Shiva K
authors: SK
authors: Kyasa
authors: M
authors: M
authors: Kannan
authors: P
authors: P
authors: Srinivas
authors: Prabhakar
authors: P
authors: Nadipalli
authors: Hira
authors: H
authors: Chaudhury
authors: V J
authors: VJ
authors: Sebastian
mesh_terms: D000620:Aminoimidazole Carboxamide / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001835:Body Weight / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D000620:Aminoimidazole Carboxamide