synthesis and activity of a new series of(z)-3-phenyl-2-benzoylpropenoic acid derivatives as aldose reductase inhibitors

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2007
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Abstract
During the course of studies directed towards the discovery of novel aldose reductase inhibitors for the treatment of diabetic complications, we synthesized a series of new (Z)-3-phenyl-2-benzoylpropenoic acid derivatives and tested their in vitro inhibitory activities on rat lens aldose reductase. Of these compounds, (Z)-3-(3,4-dihydroxyphenyl)-2-(4-methylbenzoyl)propenoicacid(3k) was identified as the most potent inhibitor, with an IC50 of 0.49μM. The theoretical binding mode of 3k was obtained by simulation of its docking into the active site of the human aldose reductase crystal structure.
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Authors ;Shao-Jie Wang;Ju-Fang Yan;Dong Hao;Xin-Wen Niu;Mao-Sheng Cheng
Journal Journal of ethnopharmacology
Year 2007
DOI
10.3390/12040885
URL
http://www.mdpi.com/1420-3049/12/4/885/
Keywords
synthesis 5 2 Organic Chemistry prodrug 5-fluorouracil structure-activity relationshipsorganic chemistry 7-triphenylquinoline

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