Rufer C, Kessler H J, Schröder E
J Med Chem. 1975 Mar;18(3):253-8. doi: 10.1021/jm00237a007.
2-(5-Nitro-2-imidazolylmethylene)-1-indanones, -1-tetralones, and -acetophenones substituted by aminoalkoxy groups and related compounds (41-69, table ii) were synthesized and their antimicrobial activities were evaluated (table iii). Some of these compounds (e.g. 47, 52, and 59) suprisingly exhibited a broad antibacterial spectrum including Proteus species and Pseudomonas aeruginosa. Extraordinary antitrichomonal activities could also be observed in vitro (MIC of compound 59, 0.0004 pg/ml) and six of the title compounds (48, 49, 52, 58, 64, 66) displayed in vivo activity in mice against Trichomonas vaginalis comparable to that of metronidazole (70).
合成了被氨基烷氧基取代的2-(5-硝基-2-咪唑基亚甲基)-1-茚酮、-1-四氢萘酮和-苯乙酮以及相关化合物(41 - 69,表ii),并评估了它们的抗菌活性(表iii)。其中一些化合物(如47、52和59)出人意料地表现出包括变形杆菌属和铜绿假单胞菌在内的广谱抗菌谱。在体外还观察到了非凡的抗滴虫活性(化合物59的MIC,0.0004 pg/ml),并且六种标题化合物(48、49、52、58、64、66)在小鼠体内对阴道毛滴虫显示出与甲硝唑相当的活性(70)。