Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378567 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
Abstract
Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with Ki = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats.
Graphical abstractDerivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine (I) were identified as potent and functionally active MCH receptor-1 (MCH-R1) antagonists. The compound 10 with Ki = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Charles Q. Huang, Tracy Baker, David Schwarz, Jun Fan, Christopher E. Heise, Mingzhu Zhang, Val S. Goodfellow, Stacy Markison, Kathleen R. Gogas, Takung Chen, Xiao-Chuan Wang, Yun-Fei Zhu,