The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives

被引：97

作者：

Bonesi, Marco ^{[1
]}

Loizzo, Monica R. ^{[1
]}

Statti, Giancarlo A. ^{[1
]}

Michel, Sylvie ^{[2
]}

Tillequin, Francois ^{[2
]}

Menichini, Francesco ^{[1
]}

机构：

[1] Univ Calabria, Dept Pharmaceut Sci, Fac Pharm Nutr & Hlth Sci, I-87030 Arcavacata Di Rende, CS, Italy

[2] Univ Paris 05, Lab Pharmacognosie, CNRS, Fac Sci Pharmaceut & Biol,UMR 8638, F-75006 Paris, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 06期

关键词：

Chalcones; Pyrazole derivatives; Hypertension; ACE; FLAVONOIDS; METALLOPEPTIDASES; HYPERTENSION; THERAPY;

D O I：

10.1016/j.bmcl.2010.01.113

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of chalcones (1-9) and pyrazoles (10-18) was prepared to investigate their potential activity as Angiotensin I-Converting Enzyme (ACE) inhibitors. Their structures were verified by elemental analysis, UV, IR, MS, H-1 NMR, C-13 NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC50 value of 0.219 mM, while the most potent pyrazole was 15 (IC50 value of 0.213 mM). (C) 2010 Elsevier Ltd. All rights reserved.

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页码：1990 / 1993

页数：4

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