期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 4, 页码 1134-1140出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.123
关键词
Farnesoid X receptor agonist; FXR; Nuclear receptor; Lead optimization; ADME; X-ray structure
Structure-guided lead optimization of recently described benzimidazolyl acetamides addressed the key liabilities of the previous lead compound 1. These efforts culminated in the discovery of 4-{(S)-2-[2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-3-fluoro-benzoic acid 7g, a highly potent and selective FXR agonist with excellent physicochemical and ADME properties and potent lipid lowering activity after oral administration to LDL receptor deficient mice. (c) 2011 Elsevier Ltd. All rights reserved.
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