Vasorelaxant activity of phthalazinones and related compounds

被引：66

作者：

del Olmo, E ^{[1
]}

Barboza, B

Ybarra, MI

López-Pérez, JL

Carrón, R

Sevilla, MA

Boselli, C

Feliciano, AS

机构：

[1] Univ Salamanca, Fac Farm, CISET, Dept Quim Farmaceut, E-37007 Salamanca, Spain

[2] Univ Nacl Tucuman, Fac Bioquim Quim & Farm, San Miguel De Tucuman, Argentina

[3] Univ Salamanca, Fac Farm, Dept Fisiol & Farmacol, E-37007 Salamanca, Spain

[4] Univ Pavia, Fac Farm, Dept Farmacol, I-27100 Pavia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

dihydrostilbenamide; phthalazinone; vasorelaxant activity; Rat aorta rings; alpha(1A); alpha(1B) and alpha(1D) sub-receptors affinity;

D O I：

10.1016/j.bmcl.2006.02.003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10(-5) M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50 = 0.43 mu M) the affinities for alpha(1A), alpha(1B) and alpha(1D) adrenergic sub-receptors were determined. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2786 / 2790

页数：5

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