| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362547 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
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.
Graphical abstractThe synthesis and SAR of tetrahydrocarboline analogs as MCH-1 antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Alan J. Henderson, Dustin Deering, James F. Grabowski, Mark Hadden, Xiaowu Jiang, Yuri Khmelnitsky, Michele Luche, Matthew D. Surman, Sharon Cheetham, Steven Vickers, Jean Viggers, Peter R. Guzzo,