2-phenoxy alkylaminothiazoles - with coronary vasodilator, analgesic, local anaesthetic activity

摘要

Cpds. of formula : and their acid-addn. salts (where R is H, opt. substd. alkyl or aryl; X, Y = H, Cl, alkyl; n is 2, 3 or 4) are coronary vasodilators, analgesics, spasmolytics and local anaesthetics, useful at a daily dose of 10-200 mg. 2-(4-Chlorophenoxyethylamino)-4-methylthiazole has an oral LD50 in mice of 57.5 mg/kg. Coronary blood-flow in the isolated rabbit heart is increased by a dose of 100 mu g to 250 mu g. A dose of 100 mu g in rats relieves indcued spasm in the duodenum. It is at least twice as potent as cocaine and procaine as a local anaesthetic.