(N)-Phenethyl-imidazole derivs. - are broad spectrum antimycotics also effective against dermatophytes and Gram positive bacteria (NL 14.12.79)

摘要

N-phenethylimidazole derivs. of formula (I) and their salts are new: (where A is -O- or -S-; R is (a) 1-8C alkyl, 2-8C alkenyl or 2-8C alkinyl; (b) 3-7C cycloaliphatic, (c) aryl or aryl 1-6C alkyl, in which the alkyl gp. is opt. substd. by one or more of halogen, NO2, CN, 1-6C alkyl, 1-6C alkoxy, 1-6C alkylthio, trihalomethyl or SO2Me; Z is opt. branched 1-5c alkylene; Y are each H, halogen, NO2, CN, 1-2C alkyl, 1-2C alkoxy; 1-2C alkylthio, trihalomethyl, -SO2Me or Ph, opt. substd. by one or more halogen atoms; n is 0 or an integer 1-5). (I) are broad spectrum antimycotics and can be used in human and veterinary medicine in the treatment of surface (external) and internal mycoses which have been caused by fungi such as Trichophyton, Epidermophyton, Microsporum and Candida. (I) are also very active against dermatophytes and can be used in the numerous cases of bacterial superinfection of mycotic injuries, being esp. effective against gram positive bacteria. (I) have high therapeutic indices (LD50/ED50) e.g. 1-(2,4-dichloro-beta-(2',4'-dichlorophenoxymethyleneoxy)phenethyl- )imidazole (Ia) has LD50 800 mg./kg. (mouse p.o.).