Synthesis of Hexahydro-<Emphasis Type="Italic">1H</Emphasis>-pyrido[3,2-<Emphasis Type="Italic">c</Emphasis>]azepines as Hypotensive Agents of Expected Calcium-Channel Blocking Activity |
| |
Authors: | Mohamed E El-Sadek Mansour Aboukull Osama I El-Sabbagh Hassan M Shallal |
| |
Institution: | (1) Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt |
| |
Abstract: | Summary.
Michael addition reaction of 3-(4-fluorophenylamino)-2-cyclohexenone and its 5,5-dimethyl derivative to the acrylonitrile derivatives
afforded the novel hexahydroquinolines. The target hexahydro-1H-pyrido3,2-c]azepine derivatives were obtained via ring enlargement of the corresponding hexahydroquinolines under Schmedt conditions.
Some novel pyrido3,2-c]azepines showed hypotensive activity in vivo on normotensive anaesthetized male adult albino rats and their effects on the ventricular contraction and auricular rate
of isolated rabbit hearts using Langendorff’s method and nefidipine as a reference drug were studied. Compounds 29 and 36 which bear some structural similarities to nefidipine exhibited the highest hypotensive activity and negative inotropic as
well as chronotropic activities. |
| |
Keywords: | , Hexahydroquinolines, Pyrido[3,2-c]azepines, Hypotensive activity, Nefidipine, |
本文献已被 SpringerLink 等数据库收录! |
|