Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 20, Pages 6154-6160Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.034
Keywords
Farnesoid X receptor; FXR; Nuclear receptor modulator; FXR X-ray co-crystal structure; GW 4064; GSK8062; GSK2324; Bile acid receptor; NR1H4
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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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