1. New octahydroquinazoline derivatives: synthesis and hypotensive activity.
- Author
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el-Sabbagh OI, Shabaan MA, Kadry HH, and Al-Din ES
- Subjects
- Animals, Antihypertensive Agents chemistry, Magnetic Resonance Spectroscopy, Male, Mass Spectrometry, Molecular Structure, Quinazolines chemistry, Rats, Spectrophotometry, Infrared, Antihypertensive Agents chemical synthesis, Antihypertensive Agents pharmacology, Quinazolines chemical synthesis, Quinazolines pharmacology
- Abstract
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 α(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., (Copyright © 2010 Elsevier Masson SAS. All rights reserved.)
- Published
- 2010
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