Wollweber H, Kölling H, Niemers E, Widdig A, Andrews P, Schulz H P, Thomas H
Arzneimittelforschung. 1984;34(5):531-42.
Anilides bearing a guanidino, thioallophanato, isothioallophanato or amidino group in the ortho position were synthesised (6) for investigations of their anthelmintic effects, and tested against sheep trichostrongylides. The most active anilides are those containing a 5-alkylthio, 5-alkylsulphinyl (alkyl = C3H7, C4H9), 5-phenylthio, 5-phenylsulphinyl or 4-phenylsulphonyloxy group, and a guanidino group substituted at both nitrogen atoms by a methoxycarbonyl group. The most active anthelmintic anilides are the form-, propion-, butyr- and methoxy-acetanilides (e.g. 60, 61, 66, 95, 100, 110). Of the guanidines unsubstituted at N' and N", the 2-guanidino-5-phenylthio-2-methoxyacetanilide (123) and the 2-guanidino-5-phenylsulphinyl-2-methoxyacetanilide (152) were more active than parbendazole. From the class of bismethoxycarbonylguanidines (6 alpha), which are also the most interesting products in terms of stability, febantel (110, Rintal) has been introduced into veterinary practice for the treatment of nematode infections in horses, cattle, sheep and swine.
合成了在邻位带有胍基、硫脲基、异硫脲基或脒基的酰苯胺类化合物（6），以研究它们的驱虫效果，并针对绵羊毛圆线虫进行了测试。活性最高的酰苯胺类化合物是那些含有5-烷硫基、5-烷基亚磺酰基（烷基 = C3H7、C4H9）、5-苯硫基、5-苯基亚磺酰基或4-苯磺酰氧基，且胍基的两个氮原子均被甲氧基羰基取代的化合物。活性最高的驱虫酰苯胺类化合物是甲酰基、丙酰基、丁酰基和甲氧基乙酰苯胺（例如60、61、66、95、100、110）。在N'和N"未被取代的胍类化合物中，2-胍基-5-苯硫基-2-甲氧基乙酰苯胺（123）和2-胍基-5-苯基亚磺酰基-2-甲氧基乙酰苯胺（152）比丙硫苯咪唑更具活性。从双甲氧基羰基胍类化合物（6α）中，也就是在稳定性方面也是最有趣的产物中，非班太尔（110，Rintal）已被引入兽医实践，用于治疗马、牛、羊和猪的线虫感染。
