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In vitro study and structure-activity relationship analysis of stilbenoid derivatives as powerful vasorelaxants: Discovery of new lead compound.

Abstract：

:The development of vasorelaxant as the antihypertensive drug is important as it produces a rapid and direct relaxation effect on the blood vessel muscles. Resveratrol (RV), as the most widely studied stilbenoid and the lead compound, inducing the excellent vasorelaxation effect through the multiple signalling pathways. In this study, the in vitro vascular response of the synthesized trans-stilbenoid derivatives, SB 1-8e were primarily evaluated by employing the phenylephrine (PE)-precontracted endothelium-intact isolated aortic rings. Herein we report trans-3,4,4'-trihydroxystilbene (SB 8b) exhibited surprisingly more than 2-fold improvement to the maximal relaxation (Rmax) of RV. This article also highlights the characterization of the aromatic protons in terms of their unique splitting patterns in 1H NMR.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Chan SY,Loh YC,Oo CW,Yam MF

doi

10.1016/j.bioorg.2020.104239

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

104239

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31536-4

journal_volume

104

pub_type

杂志文章

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