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Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Oct 15; Vol. 21 (20), pp. 6154-60. Date of Electronic Publication: 2011 Aug 11. - Publication Year :
- 2011
-
Abstract
- 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 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21890356
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.08.034