کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396318 | 1501183 | 2010 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: New octahydroquinazoline derivatives: Synthesis and hypotensive activity New octahydroquinazoline derivatives: Synthesis and hypotensive activity](/preview/png/1396318.png)
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 α1-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.
Application of Mannich reaction on 3-(4-chlorophenylamino)-5,5-dimethyl-2-cyclohexenone (1) led to the formation of octahydroquinazoline derivatives (2–21). Compounds 18, 20 and 21 showed a high hypotensive effect through their expected α1-blocking activity like the clinically used drug prazosin.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 11, November 2010, Pages 5390–5396