1260427-58-4Relevant academic research and scientific papers
5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists
Surman, Matthew D.,Freeman, Emily E.,Grabowski, James F.,Hadden, Mark,Henderson, Alan J.,Jiang, Guowei,Jiang, Xiaowu,Luche, Michele,Khmelnitsky, Yuri,Vickers, Steven,Viggers, Jean,Cheetham, Sharon,Guzzo, Peter R.
scheme or table, p. 7015 - 7019 (2010/12/29)
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.
