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Published on: May 3, 2018
5-Phenylcoumarin Derivatives: Design, Synthesis, and Vasodilatory Activity
Cheng Wang1, Youjia Li2, Ting Zhang3
1School of Medicine, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
Abstract:
In continuation of our previous efforts towards the development of coumarin derivatives with potential vasodilatory activity, 5-phenylcoumarin derivatives were designed and synthesized. Target compounds and their precursors exhibited moderately vasodilatory ability with EC50 at 2.5-49.0 μm. Docking studies also revealed the good binding mode of 7-methoxy-8-[2-(pyrrolidin-1-yl)ethoxy]-5-[2-(trifluoromethyl)phenyl]-2H-chromen-2-one (8c) with the target protein. Moreover, intermediates and the final products exhibited different fluorescent properties due to their substituent effect. These results may provide new ideas for the synthesis and application of 5-substituted coumarins.
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