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α,β-不饱和γ-内酯的亲脂性与生物活性之间的相关性。

alpha, beta-Unsaturated gamma-lactones correlations between lipophilicity and biological activity.

作者信息

Dal Pozzo A, Dansi A, Biassoni M

出版信息

Arzneimittelforschung. 1979;29(6):877-82.

PMID:582777
Abstract

A homogeneous series of alpha, beta-unsaturated gamma-lactones was prepared. Their in vitro activity against various microorganisms was quantitatively correlated, with the Hansch approach, to their lipophilicity, expressed by Rm chromatographic values. Although all the experimental results show a parabolic dependence, only in few cases the parabolic model calculated by Hansch fits to them. In most cases it was possible to find a good fitting between the ascending side of the parabola and the linear equation of Hansch. The meaning of the results and their utilization for future work are discussed.

摘要

制备了一系列结构均匀的α,β-不饱和γ-内酯。采用Hansch方法,将它们对各种微生物的体外活性与其亲脂性进行了定量关联,亲脂性用Rm色谱值表示。尽管所有实验结果均呈现抛物线依赖性,但只有少数情况下Hansch计算的抛物线模型与之拟合。在大多数情况下,可以在抛物线的上升侧与Hansch线性方程之间找到良好的拟合。讨论了结果的意义及其在未来工作中的应用。

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