Escario J A, Igea A M, Contreras M, Martinez-Fernandez A R, Claramunt R, Lopez C
Department of Parasitology, Faculty of Pharmacy, Complutense University, Madrid, Spain.
Ann Trop Med Parasitol. 1988 Jun;82(3):257-62. doi: 10.1080/00034983.1988.11812241.
Nine nitropyrazole derivatives were prepared and tested against Trichomonas vaginalis in vitro and in vivo, Entamoeba invadens in vitro and Plasmodium berghei in vivo. Three of the compounds, 4-4-nitropyrazole, 1-methyl-4-nitropyrazole and 4,4'-dinitro-1,1'-methylenedipyrazole, have an activity similar to that of metronidazole (used as the reference compound) against T. vaginalis and E. invadens after 48 hours of incubation. All the compounds tested were inactive against P. berghei.
制备了九种硝基吡唑衍生物,并对其进行了体外和体内抗阴道毛滴虫、体外抗侵袭内阿米巴以及体内抗伯氏疟原虫的测试。其中三种化合物,即4-4-硝基吡唑、1-甲基-4-硝基吡唑和4,4'-二硝基-1,1'-亚甲基二吡唑,在孵育48小时后,对阴道毛滴虫和侵袭内阿米巴的活性与甲硝唑(用作参考化合物)相似。所有测试的化合物对伯氏疟原虫均无活性。