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Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity |
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| Authors: | Mark Hadden Dustin M. Deering Alan J. Henderson Matthew D. Surman Michele Luche Yuri Khmelnitsky Steven Vickers Jean Viggers Sharon Cheetham Peter R. Guzzo |
| Affiliation: | 1. AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA;2. RenaSci Consultancy Ltd, Biocity, Nottingham, NG1 1GF, UK |
| Abstract: | A new series of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones possessing MCH-1 receptor antagonism is presented. Suzuki coupling of boronic acids with key triflate 6 allowed rapid generation of a range of analogs. The SAR of the MCH-1 receptor was explored with a variety of aryl and heterocyclic moieties. Selected compounds were studied in a five-day diet induced obese mouse model to evaluate their potential use as weight loss agents. |
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