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Molecules 2007, 12(4), 885-895; doi:10.3390/12040885

Synthesis and Activity of a New Series of(Z)-3-Phenyl-2-benzoylpropenoic Acid Derivatives as Aldose Reductase Inhibitors

1
Key Laboratory of New Drugs Design and Discovery of Liaoning Province, Shenyang Pharmaceutical University, Shenyang 110016, P.R. China
2
Drug Screening Center, Di Ao Pharmaceutical Group, Chengdu 123388, P.R. China
*
Author to whom correspondence should be addressed.
Received: 21 March 2007 / Revised: 23 April 2007 / Accepted: 23 April 2007 / Published: 30 April 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.
Keywords: (Z)-3-Phenyl-2-benzoylpropenoic acid; aldose reductase inhibitor; structure-activity relationships (Z)-3-Phenyl-2-benzoylpropenoic acid; aldose reductase inhibitor; structure-activity relationships
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Wang, S.-J.; Yan, J.-F.; Hao, D.; Niu, X.-W.; Cheng, M.-S. Synthesis and Activity of a New Series of(Z)-3-Phenyl-2-benzoylpropenoic Acid Derivatives as Aldose Reductase Inhibitors. Molecules 2007, 12, 885-895.

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