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Tetrahydrocarboline analogs as MCH-1 antagonists |
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| Authors: | Henderson Alan J Deering Dustin Grabowski James F Hadden Mark Jiang Xiaowu Khmelnitsky Yuri Luche Michele Surman Matthew D Cheetham Sharon Vickers Steven Viggers Jean Guzzo Peter R |
| Affiliation: | AMRI, 26 Corporate Circle, Albany, NY 12212-5098, USA. alan.henderson@amriglobal.com |
| Abstract: | A new series of tetrahydrocarbolines with potent MCH-1 antagonist activity were synthesized, using a conformationally constrained design approach towards optimizing pharmacokinetic properties. Two compounds from this series were progressed to a 5-day diet-induced obesity mouse screening model to evaluate their potential as weight loss agents. Both compounds produced a highly significant reduction in weight, which was attributed to their improved pharmacokinetic profile. |
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