Synthesis and Endectocidal Activity of Novel 1-(Arylsulfonyl)-1-[(trifluoromethyl)sulfonyl]methane Derivatives
作者:David I. Wickiser、Sharon A. Wilson、Daniel E. Snyder、Karl R. Dahnke、Charles K. Smith、Paul J. McDermott
DOI:10.1021/jm970678y
日期:1998.3.1
We have recently synthesized a series of novel disulfonylmethane compounds that have shown anthelmintic and insecticidal (endectocidal) activity. Several analogues have shown activity against the internal nematode Haemonchus contortus. In sheep studies, these analogues have shown 100% control of this internal parasite at a 10 mg/kg rate. In vitro activity against the biting flies, Stomoxys calcitrans
我们最近合成了一系列新型的二磺酰甲烷化合物,这些化合物已显示出驱虫和杀虫(杀虫)活性。几种类似物已显示出对抗内部线虫Haemonchus contortus的活性。在绵羊研究中,这些类似物显示出以10 mg / kg的速率可100%控制这种内部寄生虫。已经观察到针对叮咬的蝇Stomoxys calcitrans和Irema的体外活性分别低至25和2.3 ppm。仅观察到针对肝吸虫Fasciola hepatica和Trichostrongylus colubriformis的边缘活性。该系列大鼠肝脏线粒体的呼吸控制指数值表明,氧化磷酸化的解偶联是一种作用机制。化合物1被认为是治疗被寄生虫的羊的有前途的药物。