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5‐Phenylcoumarin Derivatives: Design, Synthesis, and Vasodilatory Activity
Author(s) -
Wang Cheng,
Li Youjia,
Zhang Ting,
Wei Di,
Hou Yajing,
He Huaizhen
Publication year - 2018
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201800255
Subject(s) - chemistry , substituent , coumarin , vasodilation , stereochemistry , alkoxy group , trifluoromethyl , docking (animal) , combinatorial chemistry , organic chemistry , medicine , alkyl , nursing , cardiology
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 EC 50 at 2.5–49.0 μ m . Docking studies also revealed the good binding mode of 7‐methoxy‐8‐[2‐(pyrrolidin‐1‐yl)ethoxy]‐5‐[2‐(trifluoromethyl)phenyl]‐2 H ‐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.