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稠合[1,4]苯并噻嗪和[1,5]苯并硫氮杂䓬的研究,V. 4,5-二氢-s-三唑并[3,4-d]-1,5-苯并硫氮杂䓬的N-2-烷基氨基衍生物的合成与生物活性

Studies on annelated [1,4]benzothiazines and [1,5]benzothiazepines, V. Synthesis and biological activity of N-2 alkylamino derivatives of 4,5-dihydro-s-triazolo[3,4-d]-1,5-benzothiazepine.

作者信息

Ambrogi V, Giampietri A, Grandolini G, Perioli L, Ricci M, Tuttobello L

机构信息

Istituto di Chimica Farmaceutica e Tecnica Farmaceutica, Università degli Studi di Perugia, Italy.

出版信息

Arch Pharm (Weinheim). 1992 Sep;325(9):569-77. doi: 10.1002/ardp.19923250909.

Abstract

The synthesis of a new series of N-2 alkylamino derivatives of 4,5-dihydro-s-triazolo[3,4-d]-1,5-benzothiazepine has been accomplished starting from 2,3-dihydro-1,5-benzothiazepin-4(5H)ones and their 2-methyl and 2-aryl derivatives. All the compounds were tested in vitro for their antimicrobial activity, but none of them showed remarkable activity. The tricyclic compounds 7a-j, 8a-j, 9a-j, 10a-j, and 11a-j were also screened for their CNS activity in mice and several of them showed interesting activity.

摘要

从2,3-二氢-1,5-苯并硫氮杂䓬-4(5H)酮及其2-甲基和2-芳基衍生物出发,完成了一系列新的4,5-二氢-s-三唑并[3,4-d]-1,5-苯并硫氮杂䓬的N-2烷基氨基衍生物的合成。所有化合物均进行了体外抗菌活性测试,但均未显示出显著活性。还对三环化合物7a-j、8a-j、9a-j、10a-j和11a-j在小鼠体内的中枢神经系统活性进行了筛选,其中几种显示出有趣的活性。

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