Synthesis Character and Structure-Activity Study of Novel Fasciolicides

摘要

The parasite fasciola hepatica is very damaging to animal husbandry in all over the world. It causes huge economic losses annually especially in those countries that stock raising is the dominating support to national economy. So the successful treatment of fasciolosis is very important to the society. However most anthelmintic-active drugs are only effective against adult Ever fluke and some which were formerly effective against immature parasite have now lost their advantage in the chemoprophylaxis of fasciolosis due to the development of drag resistance. We tried to find a new kind of drags which is more effective against both adult and immature fasciola hepatica. basing on our previous structure-activity relationship studies we synthesized a new series of fasciolicides- hydroxylbenzendisulfonanilides. Structures of the compounds were characterized by IR and ~1HNMR. and their physical properties were determined through UV and high- performance liquid chromatography (HPLC). We also examined their uncoupling activity of oxidative phosphorylation in mitochondria comparing with N-(2 ' ,4 ' , 5 ' -trichlorine) phenyl-2-hydroxyl -3, 5, 6-trichlorinbenzensulfonanilide (HBSA), Literatures reported that HBSA. is a strong uncoupler of oxidative phosphorylation in mitochondria and a potent fasciolicides to the adult and immature liver flukes.