Verge J P, Roffey P
J Med Chem. 1975 Aug;18(8):794-7. doi: 10.1021/jm00242a007.
A series of 2-(5-nitro-2-thienyl)thiazoles and their vinylogs having substituted methylamine side chains has been prepared by halogen displacement on the corresponding 4-chloromethylthiazole. Of these, 4-morpholinomethyl-2-(5-nitro-2-thienyl)thiazole showed moderate activity against Trypanosoma cruzi and Trypanosoma rhodesiense in mice. This compound formed the lead for a series of analogous thiazole-4-carboxaldehyde hydrazones. Some of the latter were found active in curing murine Tryp. cruzi and Tryp. rhodesiense infections and to have low acute toxicity. A comparison with known active compounds is given and some structural features necessary for activity are discussed.
通过对相应的4-氯甲基噻唑进行卤素取代反应，制备了一系列带有取代甲胺侧链的2-(5-硝基-2-噻吩基)噻唑及其插烯物。其中，4-吗啉甲基-2-(5-硝基-2-噻吩基)噻唑对小鼠体内的克氏锥虫和罗德西亚锥虫显示出中等活性。该化合物成为了一系列类似噻唑-4-甲醛腙的先导化合物。发现其中一些对治疗小鼠克氏锥虫和罗德西亚锥虫感染具有活性，且急性毒性较低。文中给出了与已知活性化合物的比较，并讨论了活性所需的一些结构特征。
