| Literature DB >> 17107792 |
Roger A Smith1, Zahra Fathi, Su-Ellen Brown, Soongyu Choi, Jianmei Fan, Susan Jenkins, Harold C E Kluender, Anish Konkar, Rico Lavoie, Ronald Mays, Jennifer Natoli, Stephen J O'Connor, Astrid A Ortiz, Brent Podlogar, Christy Taing, Susan Tomlinson, Theresa Tritto, Zhonghua Zhang.
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 Ki and Kb values below 10 nM, 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.Entities:
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Year: 2006 PMID： 17107792 DOI： 10.1016/j.bmcl.2006.10.095
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823