Rational Design, Synthesis, Biological Evaluation, Homology and Docking Studies of Coumarin Derivatives as α1??Adrenoceptor Antagonists

X Zhou, YD Chen, T Wang, XB Wang…

Index: Zhou, Xiang; Chen, Ya-Dong; Wang, Tao; Wang, Xiao-Bing; Kong, Ling-Yi Chemistry and Biodiversity, 2011 , vol. 8, # 6 p. 1052 - 1064

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Abstract

Abstract According to a three-point pharmacophore for some uro-selective α 1-adrenoceptor (AR) antagonists, a novel class of coumarin (= 2H-1-benzopyran-2-one) derivatives have been successfully designed and synthesized with high efficacies for α 1-AR. These synthesized coumarin derivatives exhibited high efficacies towards α 1-AR in in vitro pharmacological assays. Compared with prazosin (pK i value of 8.77), among those ...