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Synthesis and structure-activity relationships of 2-(4-benzhydryl-1-piperazinyl)-1-phenylethanols as new calcium
Y Nomura1, T Yamakawa, K Nishioka
1Department of Applied Chemistry, Faculty of Engineering, Saitama University, Japan.
Abstract:
A series of 2-(4-benzhydryl-1-piperazinyl)-1-phenylethanols (4) was synthesized and evaluated for calcium entry-blocking activity, assessed as inhibitory activity on calcium current in rat hippocampal pyramidal neurons by using a patch-clamp technique (10(-5) M), and cerebral vasodilating activity, assessed in terms of increase of vertebral blood flow after intravenous administration (1 mg/kg) in anesthetized dogs. Alkoxy substituents on the phenyl ring of the phenylethanol moiety conferred potent calcium entry-blocking activity and potent cerebral vasodilating activity. Among these compounds, 4i (NC-1100) was selected as the best analog. Some pharmacological properties of 4i are presented.