具有抗痉挛活性γ-(4-取代哌嗪-1-基)-α-苯基丙醇不对称酯衍生物的合成

P. O. Osadebe, P. Akah, C. O. Okafor, L. Natova
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引用次数: 0

摘要

通过对γ-(4-取代哌嗪基)-α-苯基丙醇的酯化反应,制备了6个新的酯类衍生物。这些衍生物分别为甲酯、乙酯、苯酯和苄酯,采用固-液相转移催化酯化法,产率较高。测定了新衍生物的含氮量。用离体豚鼠回肠进行的研究表明,这些衍生物具有不同程度的抗痉挛活性。其中,γ-(4-苄基哌嗪-1-酰基)-α-苯基丙醇乙酯的抗痉挛活性最强。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of Some Unsymmetrical Ester Derivatives of γ-(4-Substituted piperazin-1-yl)-α-phenyl propanols with Antispasmodic Activity
Six new ester derivatives of γ-(4-substituted piperazinyl)-α-phenyl propanol were prepared by esterification of the γ-piperazinyl propanols. The derivatives were methyl, ethyl, phenyl and benzyl esters, and they were obtained in good yields using a solid-liquid phase transfer catalysed esterification method. The nitrogen content of the new derivatives was also determined. Studies using isolated guineapig ileum showed that the derivatives possessed varying degrees of antispasmodic activity. Of the compounds evaluated, the ethyl ester of γ-(4-benzyl piperazin-1-yl)-α-phenyl propanol showed the greatest antispasmodic activity.
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