抗炎症薬に関する研究(第1報) : Thienopyridine誘導体の生物活性

抄録

6-Substituted-2-amino-3-ethoxycarbonyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridines were examined for their anti-edematous and analgesic activity. Derivatives substituted in 6-position with methyl (II), n-butyl (III), n-octyl (IV), allyl (V), propargly (VI), benzyl (VIII), phenethyl (X), and acetyl (XI), as well as 6-unsubstituted compound (I), were more active against carrageenin-induced rat paw edema than acetylsalicylic acid or aminopyrine. By oral administration of 250mg/kg of I, II, V and VI some rats died from the toxicity. In Randall-Selitto test, VIII and XI showed most potent analgesic activity. 6-Cyclohexyl (VII), (III), and (X) were more active than aminopyrine, and IV and 6-p-chlorobenzyl (IX) than acetylsalicylic acid which has weaker analgesic activity than aminopyrine. VIII also revealed potent activity in benzoquinone-induced writhing test in mice. VIII may serve as analgesics and anti-inflammatory agents.