Citation: . Design, synthesis and metabolic regulation effect of farnesoid X receptor (FXR) antagonistic benzoxepin-5-ones[J]. Chinese Chemical Letters, ;2017, 28(7): 1519-1522. doi: 10.1016/j.cclet.2017.04.034 shu

Design, synthesis and metabolic regulation effect of farnesoid X receptor (FXR) antagonistic benzoxepin-5-ones

Received Date: 6 March 2017
Revised Date: 10 April 2017
Accepted Date: 28 April 2017
Available Online: 6 July 2017

Figures(5)

A series of benzoxepin-5-ones were designed and synthesized by the cyclization of chalcones which were previously found as FXR antagonists. The cellular FXR antagonism of benzoxepines was investigated, among which the most potent compound 10l was able to reduce the plasma and hepatic triglyceride and plasma ALT levels in mice.
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