title: Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists.
abstract: Since the CB1 receptor antagonist SR141716 (rimonabant) was reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target in the treatment of obesity. Several series of derivatives based on diarylimidazolyl oxadiazole and thiadiazole scaffolds were synthesized and tested for CB1 receptor binding affinity. SAR studies directed toward the optimization of imidazole scaffolds resulted in the discovery of 10s which showed highest potency for CB1 receptor binding affinity (IC(50)=1.91nM) prepared to date.
authors.affiliation: Central Research Laboratories, Green Cross Corporation, Yongin, Gyeonggi-Do, Republic of Korea.
authors.forename: Jong Yup
authors.initials: JY
authors.lastname: Kim
authors.forename: Hee Jeong
authors.initials: HJ
authors.lastname: Seo
authors.forename: Sung-Han
authors.initials: SH
authors.lastname: Lee
authors.forename: Myung Eun
authors.initials: ME
authors.lastname: Jung
authors.forename: Kwangwoo
authors.initials: K
authors.lastname: Ahn
authors.forename: Jeongmin
authors.initials: J
authors.lastname: Kim
authors.forename: Jinhwa
authors.initials: J
authors.lastname: Lee
mesh_terms: D000818:Animals; D007093:Imidazoles; D020128:Inhibitory Concentration 50; D009765:Obesity / Q000188:drug therapy; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D007093:Imidazoles; D010069:Oxadiazoles; D043884:Receptor, Cannabinoid, CB1; D013830:Thiadiazoles