期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 20, 页码 6154-6160出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.034
关键词
Farnesoid X receptor; FXR; Nuclear receptor modulator; FXR X-ray co-crystal structure; GW 4064; GSK8062; GSK2324; Bile acid receptor; NR1H4
To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene If and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency. (C) 2011 Elsevier Ltd. All rights reserved.
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