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新型1-取代-1'-甲基-3-氯-2-氧代螺(氮杂环丁烷-3',4-吲哚-2'酮)的合成与抗惊厥活性

Synthesis and anticonvulsant activity of new 1-substituted 1'-methyl-3-chloro-2-oxospiro (azetidin-3',4-indol-2' ones).

作者信息

Singh G S, Siddiqui N, Pandeya S N

机构信息

Department of Pharmaceutics, Banaras Hindu University, Varanasi, India.

出版信息

Boll Chim Farm. 1994 Feb;133(2):76-9.

PMID:8003285
Abstract

The aim of the present research work is to discover new compounds with potential anticonvulsant activity. Several indolinone derivatives and also azetidinones are reported to have significantly anticonvulsant activity. So, it was thought considerable to synthesise compounds having both these moieties and study their anticonvulsant activity. The new spiroazetinones synthesized from the reaction of 3-(N-substituted) imino-1-methyl-indol-2-ones with chloroacetyl chloride in presence of triethylamine have been characterised on the basis of triethylamine have been characterised on the basis of satisfactory analytical and spectral data. Of the eight compounds screened in the series two compounds (3c and 3h) exhibited significant activity against MES.

摘要

本研究工作的目的是发现具有潜在抗惊厥活性的新化合物。据报道,几种吲哚啉酮衍生物以及氮杂环丁烷酮具有显著的抗惊厥活性。因此,人们认为合成同时含有这两个部分的化合物并研究它们的抗惊厥活性是很有意义的。由3-(N-取代)亚氨基-1-甲基吲哚-2-酮与氯乙酰氯在三乙胺存在下反应合成的新型螺氮杂环丁烷酮,已根据令人满意的分析和光谱数据进行了表征。在该系列筛选的八种化合物中,有两种化合物(3c和3h)对最大电休克(MES)表现出显著活性。

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