کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362545 | 981490 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
The synthesis and SAR of 5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as potent MCH-1 antagonists are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7015–7019
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7015–7019
نویسندگان
Matthew D. Surman, Emily E. Freeman, James F. Grabowski, Mark Hadden, Alan J. Henderson, Guowei Jiang, Xiaowu (May) Jiang, Michele Luche, Yuri Khmelnitsky, Steven Vickers, Jean Viggers, Sharon Cheetham, Peter R. Guzzo,