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

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Abstract
A number of 5,6,7,8-tetrahydroquinoline-8-nitriles and -8-thioamides and related compounds are 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 proved useful in determining factors necessary for such activity and structure-activity relationships are discussed. The most necessary requirements for activity are a pyridine N with its available lone pair and a primary or secondary thioamide. Also desirable is a 6-membered carbocyclic ring with relative freedom from steric hinderance around the 8 position.