New octahydroquinazoline derivatives: Synthesis and hypotensive activity

被引：32

作者：

El-Sabbagh, O. I. ^{[1
]}

Shabaan, Mohamed A. ^{[2
]}

Kadry, Hanan H. ^{[2
]}

Al-Din, Ehab Saad ^{[3
]}

机构：

[1] Zagazig Univ, Fac Pharm, Dept Med Chem, Zagazig, Egypt

[2] Cairo Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Cairo, Egypt

[3] Al Azhar Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Assiut, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期

关键词：

Synthesis; Octahydroquinazoline derivatives; Hypotensive activity; ANTIHYPERTENSIVE ACTIVITY; ANTAGONISTS; PRESSURE; ANALOGS; AGENTS;

D O I：

10.1016/j.ejmech.2010.08.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several novel 1-(4-chlorophenyl)-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydro-5-oxo-3-(substitutedphenyl) quinazoline derivatives (2-21) structurally similar to prazosin, were prepared using Mannich reaction of 3-(4-chlorophenylamino)-5,5-dimethyl-2-cyclohexenone (1) with different aromatic amines in the presence of formaline. The structures of the quinazoline derivatives were established using elemental and spectral analyses. Compounds 18, 20 and 21 were found to possess a high hypotensive effect through their expected alpha(1)-blocking activity like the clinically used drug prazosin but with advantageous of being did not cause reflex tachycardia and having prolonged duration of action when tested in adrenaline-induced hypertension in anaesthetized rats. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：5390 / 5396

页数：7

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