Ross W J, Jamieson W B
J Med Chem. 1975 Apr;18(4):430-2. doi: 10.1021/jm00238a022.
A series of 2-styryl-5-nitro-1-vinylimidazoles carrying alkylaminomethyl or amidino functions in the 4 position of the styryl ring was prepared and evaluated for antitrypanosomal activity in mice infected with Trypanosoma rhodesiense. The alkylaminomethyl compounds were found inactive against Trypanosoma cruzi infections in mice. One compound, 2-(4-methylamidinostyryl)-5-nitro-1-vinylimidazole hydrochloride, showed antitrypanosomal activity comparable to the standard drugs suramin, pentamidine, diminazene, and melarsoprol when tested ip against T. rhodesiense infected mice and also showed some activity when tested ip against T. cruzi infected mice.
制备了一系列在苯乙烯基环的4位带有烷基氨基甲基或脒基官能团的2-苯乙烯基-5-硝基-1-乙烯基咪唑，并在感染了罗德西亚锥虫的小鼠中评估其抗锥虫活性。发现烷基氨基甲基化合物对小鼠的克氏锥虫感染无活性。一种化合物，2-(4-甲基脒基苯乙烯基)-5-硝基-1-乙烯基咪唑盐酸盐，经腹腔注射测试，对感染罗德西亚锥虫的小鼠显示出与标准药物苏拉明、喷他脒、二脒那秦和美拉胂醇相当的抗锥虫活性，经腹腔注射测试，对感染克氏锥虫的小鼠也显示出一定活性。
