Synder H R, Bird L L, Siedler A J, Anderson J
J Med Chem. 1975 Sep;18(9):942-5. doi: 10.1021/jm00243a016.
A series of 1-[[(5-nitrofuranyl)methylene]amino]-4- and/or -5-substituted 2-imidazolidinones was prepared utilizing three different reaction sequences. The structure of 4, the product derived from 4-methyl-2-imidazolidinone (2a), was verified by synthesis using an alternate, unequivocal route. The levo isomer l-4 was prepared by a series of reactions starting with L(+)-2-amino-1-propanol (l-10). All of the nitrofurans were examined for potential use as chemotherapeutic agents for urinary tract infections. Based on the high level of activity in the urine and the in vitro antibacterial activity (MIC) 4, l-4, and 16 are considered to be the most active as urinary tract agents.
利用三种不同的反应序列制备了一系列1-[[(5-硝基呋喃基)亚甲基]氨基]-4-和/或-5-取代的2-咪唑啉酮。通过使用另一种明确的路线合成，验证了由4-甲基-2-咪唑啉酮(2a)衍生的产物4的结构。左旋异构体l-4是通过一系列从L(+)-2-氨基-1-丙醇(l-10)开始的反应制备的。对所有硝基呋喃进行了检查，看其是否有作为尿路感染化疗药物的潜在用途。基于尿液中的高活性水平和体外抗菌活性(MIC)，4、l-4和16被认为是作为尿路药物最具活性的。
