具有降压活性的N'-酰基-N,N-(1,3,3-三甲基双环[2.2.1]庚-2-亚基)苯甲脒类化合物。

N'-acyl-N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidines with hypotensive activity.

作者信息

Bondavalli F, Bruno O, Schenone P, Filippelli W, Russo S, Marmo E

出版信息

Farmaco Sci. 1987 May;42(5):335-40. doi: 10.1002/chin.198748161.

DOI:10.1002/chin.198748161

Abstract

The reaction of fenchone nitrimine (I) with benzamidine gave in good yield N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidine (II), which by acylation afforded N'-acyl-N,N-(1,3,3-trimethylbicyclo[2.2.1]hept-2-ylidene)benzam idines (III a-f) in excellent yields. Compounds (III) showed a moderate hypotensive activity in rats and a weak local anesthetic activity by infiltration in mice. Effects on heart rate and antiarrhythmic activity in rats are also reported.

摘要

葑酮硝酮（I）与苯甲脒反应，以良好的产率得到N，N-（1,3,3-三甲基双环[2.2.1]庚-2-亚基）苯甲脒（II），其经酰化反应以优异的产率得到N'-酰基-N，N-（1,3,3-三甲基双环[2.2.1]庚-2-亚基）苯甲脒（III a-f）。化合物（III）在大鼠中表现出中等程度的降压活性，在小鼠中通过浸润表现出较弱的局部麻醉活性。还报道了对大鼠心率和抗心律失常活性的影响。

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