异构噻吩并[1,4]苯并噻嗪的合成与抗精神病活性

Synthesis and neuroleptic activity of isomeric thieno(1,4)benzothiazines.

作者信息

Grol C J, Rollema H

出版信息

J Med Chem. 1975 Aug;18(8):857-61. doi: 10.1021/jm00242a023.

DOI:10.1021/jm00242a023

Abstract

To investigate the influence of electronic properties of the tricyclic thiazine system on neuroleptic activity, a series of the isomeric N-dimethylaminopropylthienobenzothiazines was synthesized. All compounds were screened for neuroleptic activity in mice and rats. For the active compounds lowest active doses in the antiamphetamine test were determined. Activity appeared to be dependent on the mode of annelation of the thiophene molecule: compunds bearing the same substituent and side chain with the thiophene molecule in 2,3 and 3,4 annelation were active, while those compounds with a 3,2 annelation seemed to be devoid of activity at the given dose.

摘要

为研究三环噻嗪系统的电子性质对抗精神病活性的影响，合成了一系列异构的N - 二甲基氨基丙基噻吩并苯并噻嗪。所有化合物均在小鼠和大鼠中进行了抗精神病活性筛选。对于活性化合物，测定了其在抗苯丙胺试验中的最低有效剂量。活性似乎取决于噻吩分子的稠合方式：在2,3和3,4稠合中带有相同取代基和侧链的噻吩分子的化合物具有活性，而在给定剂量下，具有3,2稠合的那些化合物似乎没有活性。

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