942435-72-5Relevant academic research and scientific papers
Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists
Kim, Jong Yup,Seo, Hee Jeong,Lee, Sung-Han,Jung, Myung Eun,Ahn, Kwangwoo,Kim, Jeongmin,Lee, Jinhwa
body text, p. 142 - 145 (2009/05/30)
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 an
CB1 RECEPTOR MODULATORS
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, (2010/01/12)
Compounds of formula (I) suppress the normal signalling activity of cannabinoid receptor CB1 and are therefore useful inter alia in the treatment of conditions directly or indirectly associated with obesity and overweight, Wherein A1 is -COOH o
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity
Smith, Roger A.,Fathi, Zahra,Achebe, Furahi,Akuche, Christiana,Brown, Su-Ellen,Choi, Soongyu,Fan, Jianmei,Jenkins, Susan,Kluender, Harold C.E.,Konkar, Anish,Lavoie, Rico,Mays, Ronald,Natoli, Jennifer,O'Connor, Stephen J.,Ortiz, Astrid A.,Su, Ning,Taing, Christy,Tomlinson, Susan,Tritto, Theresa,Wang, Gan,Wirtz, Stephan-Nicholas,Wong, Wai,Yang, Xiao-Fan,Ying, Shihong,Zhang, Zhonghua
, p. 2706 - 2711 (2008/12/20)
Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provided the imidazole 2-hydroxy-cyclohexyl amide 45, which exhibited hCB-1 Ki = 3.7 nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models.
