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

被引：90
|
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.
引用
收藏
页码：1990 / 1993
页数：4
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