具有潜在抗溃疡和/或抗分泌活性的双环化合物。I. 4,5,6,7-四氢苯并咪唑类

Bicyclic compounds with potential antiulcer and/or antisecretory activity. I. 4,5,6,7-Tetrahydrobenzimidazoles.

作者信息

Scarponi U, Cimaschi R, Rusconi L, Santangelo F, Arcari G, Castello R, Toti D, de Castiglione R

出版信息

Farmaco Sci. 1985 Nov;40(11):818-32.

Abstract

The remarkable antiulcer and antisecretory activity of some previously described 4,5,6,7-tetrahydroimidazo[4,5-c]pyridine derivatives prompted us to further investigate related bicyclic systems. Accordingly, a series of 5-amino- and 5-aminomethyl-4,5,6,7-tetrahydrobenzimidazoles, regiospecifically alkylated in position 1, were synthesized and tested. Only a few 1-ethyl-5-amino derivatives displayed a reasonable antiulcer activity in comparison with our former class of compounds.

摘要

一些先前描述的4,5,6,7-四氢咪唑并[4,5-c]吡啶衍生物具有显著的抗溃疡和抗分泌活性，这促使我们进一步研究相关的双环体系。因此，我们合成并测试了一系列在1位进行区域特异性烷基化的5-氨基-和5-氨甲基-4,5,6,7-四氢苯并咪唑。与我们之前的一类化合物相比，只有少数1-乙基-5-氨基衍生物表现出合理的抗溃疡活性。

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