作者
Matthew D Surman, Emily E Freeman, James F Grabowski, Mark Hadden, Alan J Henderson, Guowei Jiang, Michele Luche, Yuri Khmelnitsky, Steven Vickers, Jean Viggers, Sharon Cheetham, Peter R Guzzo
发表日期
2010/12/1
期刊
Bioorganic & medicinal chemistry letters
卷号
20
期号
23
页码范围
7015-7019
出版商
Pergamon
简介
A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl)indazoles to give 5-(furopyridinon-5-yl)indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy.
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MD Surman, EE Freeman, JF Grabowski, M Hadden… - Bioorganic & medicinal chemistry letters, 2010