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4-(3-氧代-1,2-苯并异噻唑啉-2-基)苯基链烷酸衍生物的合成与镇痛活性

[Synthesis and analgesic activity of 4-(3-oxo-1,2-benzoisothiazoline-2-yl)phenylalkanoic derivatives].

作者信息

Plazzi P V, Bordi F, Vitali F, Silva C, Chiavarini M, Morini G, Impicciatore M

出版信息

Farmaco Sci. 1984 Sep;39(9):788-96.

PMID:6500045
Abstract

The synthesis of a new series of 4-(3-oxo-1,2-benzisothiazolin-2-yl)phenylalkanoic compounds and some of their functional derivatives is described. The compounds, on the basis of data obtained from 1,2-benzisothiazolin-3-one derivatives, were biologically examined mainly for their antiphlogistic and analgesic actions. Results obtained, in analyzing the relationship between structure and pharmacological actions, suggest that both 4-(3-oxo-1,2-benzisothiazolin-2-yl)-phenyalkanoic acids and o-sulphobenzimido alkanoic esters are endowed with pain-killing effects comparable in potency and efficacy with phenylbutazone.

摘要

本文描述了一系列新的4-(3-氧代-1,2-苯并异噻唑啉-2-基)苯基链烷酸化合物及其某些功能衍生物的合成。基于从1,2-苯并异噻唑啉-3-酮衍生物获得的数据,对这些化合物主要进行了抗炎和镇痛作用的生物学研究。在分析结构与药理作用之间的关系时所获得的结果表明,4-(3-氧代-1,2-苯并异噻唑啉-2-基)苯基链烷酸和邻磺基苯甲酰亚胺链烷酸酯均具有与保泰松相当的止痛效力和效果。

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