2. Academic Validation
  3. Tetrahydrocarboline analogs as MCH-1 antagonists

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.
Alan J Henderson 1,  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
Affiliations

Affiliation

  • 1 AMRI, 26 Corporate Circle, Albany, NY 12212-5098, USA. alan.henderson@amriglobal.com
PMID: 20952195 DOI: 10.1016/j.bmcl.2010.09.122
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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