| 摘要 |
<p>Thiazolo-isoquinolines of formula (I), in (R) or (S) forms or their mixts. and their acid addition salts are new. In the formula, X1=H, halo, CH3O or CN. X2=H, halo or CH3O; or X1 + X2 = methylenedioxy. Y1 and Y2 = H, halo, 1-4C alkyl, alkoxy or alkylthio, OH diacetylamino or NH2. They are prepd. e.g. by acid cyclisation of 2-(pyridylaminothiocarbonyl). 3-hydroxymethyl-tetrahydroisoquinoline. (I) are anti-ulcer agents e.g. they antagonise the histamine-induced gastric acid secretion at 10-50 mg/kg orally and some are effective against experimentally-induced gastric ulcers at 20-100 mg/kg. Toxicity is >=100 mg/kg orally and most show no signs of toxicity at 900 mg/kg orally in mice. A typical cpd. is (5)-3-(2-pyridylimino)-1,5,10,10a-tetrahydrothiazolo 3,4,b isoquinoline.</p> |
