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Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.

作者信息

Ellsworth Bruce A, Wang Ying, Zhu Yeheng, Pendri Annapurna, Gerritz Samuel W, Sun Chongqing, Carlson Kenneth E, Kang Liya, Baska Rose A, Yang Yifan, Huang Qi, Burford Neil T, Cullen Mary Jane, Johnghar Susan, Behnia Kamelia, Pelleymounter Mary Ann, Washburn William N, Ewing William R

机构信息

Pharmaceutical Research Institute, Bristol Myers Squibb Co., PO Box 5400 Princeton, NJ 08543, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. doi: 10.1016/j.bmcl.2007.04.087. Epub 2007 Apr 29.

DOI:10.1016/j.bmcl.2007.04.087
PMID:17513109
Abstract

Structure-activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose.

摘要

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