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Your search keyword '"Lavoie Rico"' showing total 2 results
Start Over Author "Lavoie Rico" Topic cannabinoid
2 results on '"Lavoie Rico"'

1. Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity

Author

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, and Wang, Gan

Subjects
*AMIDES, *CANNABINOIDS, *OBESITY treatment, *HUMAN body composition
Abstract

Abstract: 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 K i =3.7nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models. [Copyright &y& Elsevier]

Published
2007
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2. Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives

Author

Smith, Roger A., Fathi, Zahra, 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., Podlogar, Brent, Taing, Christy, Tomlinson, Susan, Tritto, Theresa, and Zhang, Zhonghua

Subjects
*KETONES, *PYRIDINE, *BIOSYNTHESIS, *PYRAZOLES
Abstract

Abstract: A series of pyrrolopyridinones was designed and synthesized as constrained analogs of the pyrazole CB-1 antagonist rimonabant. Certain examples exhibited very potent hCB-1 receptor binding affinity and functional antagonism with K i and K b values below 10nM, and with high selectivity for CB-1 over CB-2 (>100-fold). A representative analog was established to cause significant appetite suppression and reduction in body weight gain in industry-standard rat models used to develop new therapeutics for obesity. [Copyright &y& Elsevier]

Published
2007
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