5,6,7,8-四氢喹啉。4. 5,6,7,8-四氢喹啉腈和硫代酰胺的抗溃疡和抗分泌活性。

5,6,7,8-Tetrahydroguinolines. 4. Antiulcer and antisecretory activity of 5,6,7,8-tetrahydroquinolinenitriles and -thioamides.

作者信息

Beattie D E, Crossley R, Curran A C, Dixon G T, Hill D G, Lawrence A E, Shepherd R G

出版信息

J Med Chem. 1977 May;20(5):714-8. doi: 10.1021/jm00215a019.

Abstract

A number of 5,6,7,8-tetrahydroquinoling-8-nitriles and -8-thioamides and related compounds have been found to be potent inhibitors of basal gastric secretion in the pylorus-ligated rat and to afford protection against gastric erosions induced in rats by cold-restraint stress. Molecular manipulation has proved useful in determining factors necessary for such activity and structure-activity relationships are discussed. It has been shown that the most necessary requirements for activity are a pyridine nitrogen with its available lone pair and a primary or secondary thioamide. Also desirable is a six-membered carbocyclic ring with relative freedom from steric hinderance around the 8 position.

摘要

已发现多种5,6,7,8 - 四氢喹啉 - 8 - 腈和 - 8 - 硫代酰胺以及相关化合物是幽门结扎大鼠基础胃酸分泌的有效抑制剂，并能保护大鼠免受冷束缚应激诱导的胃糜烂。分子操作已被证明有助于确定这种活性所需的因素，并讨论了构效关系。结果表明，活性最必要的要求是带有可用孤对电子的吡啶氮和伯或仲硫代酰胺。还需要一个六元碳环，8位周围相对没有空间位阻。