title: Recent advances in CB1 cannabinoid receptor antagonists.
abstract: Cannabinoid CB1 receptor antagonists are currently the subject of intensive research due to their highly promising therapeutic prospects. Novel chemical entities having CB1 antagonistic properties have recently been disclosed by several pharmaceutical companies and some academic research groups, some of which are close structural analogs of the leading compound rimonabant (SR-141716A; Sanofi-Synthélabo). A considerable number of these CB1 antagonists are bioisosteres that are derived from rimonabant by the replacement of the pyrazole moiety with an alternative heterocycle. As well as these achiral compounds, Solvay Pharmaceuticals have disclosed a novel class of chiral pyrazolines that are potent and CB1/CB2 subtype-selective cannabinoid receptor antagonists, in which the interactions with the CB1 receptor are highly stereoselective.
authors.affiliation: Solvay Pharmaceuticals, Research Laboratories, CJ van Houtenlaan 36, 1381 CP, Weesp, the Netherlands. jos.lange@solvay.com
authors.forename: Jos H M
authors.initials: JH
authors.lastname: Lange
authors.forename: Chris G
authors.initials: CG
authors.lastname: Kruse
mesh_terms: D000818:Animals; D017326:Clinical Trials, Phase III as Topic; D006801:Humans; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000187:drug effects* / Q000627:therapeutic use; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000187:drug effects; D000077285:Rimonabant; D012680:Sensitivity and Specificity
chemical_list: D010880:Piperidines; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D000077285:Rimonabant