| 摘要 |
Cpds. of formula (I) and their salts are new: In (I) R is 1-6C alkyl, Y is -NR1R2, -NR1-CO-R1, -NR1-CO-NHR2, -NR1-CO-OR2 or -SO2R2, R1 and R2 are each H or 1-6C alkyl, R1 is (a) 1-12c alkyl opt. substd. by >=1 halogen, CN carboxyl, carbamyl, -SEt, -OR1, -NR1R2 or Ph (opt. substd by >=1 OH) gps. or is (b) Ph opt. substd. by >=1 halogen, CN, 1-6C alkyl, 1-6C trihaloalkyl, NO2, -OR1 or -NR1R2 gps. R2 is 1-4C alkyl. (I) are useful in human and veterinary medicine as antiamoebic agents. Activity is higher than previously used dichloroacetamide derivs. Useful for treating intestinal infections caused by Entamoeba histolytica in acute and chronic cases, as well as in prophylaxis where the agent is endemic LD50 is e.g. >800 mg/kg p.p. Adult doses are e.g. 200-1000 mg (pref. 200-500 mg) p.o. 1-3 times/day over 5-10 days. |
