Tetrahydrocarboline analogs as MCH-1 antagonists
- Bioorg Med Chem Lett. 2010 Dec 1;20(23):7024-8. doi: 10.1016/j.bmcl.2010.09.122.
- 1. AMRI, 26 Corporate Circle, Albany, NY 12212-5098, USA. [email protected]
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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