新型抗肝片吸虫病药物化合物HBSA-CO1的合成及解偶联活性研究  

The Synthesis of the New Drug Compound (HBSA-CO1) Against Parasite Fasciola Hepatica and Study on the Uncoupling Activity

作　　者：王晓晶[1] 赵军[1] 李哲[1] 陈静[1] 石玉[1] 新民[1] 

机构地区：[1]内蒙古大学化学系,内蒙古呼和浩特010021

出　　处：《内蒙古大学学报（自然科学版）》2000年第2期177-180,共4页Journal of Inner Mongolia University：Natural Science Edition

基　　金：国家自然科学基金!(项目批准号29622001)

摘　　要：合成了邻羟基苯磺酰苯胺类药物化合物 :N ( 2 ,5 二甲基 4 苯甲酰基 )苯基 2 羟基 3 ,5,6 三氯苯磺酰胺 (HBSA CO1 ) ,并对该药物化合物进行了结构表征 .采用氧电极法、测呼吸过程中磷的变化以及测ATP酶活性等方法研究其对线粒体氧化磷酸化反应的解偶联作用 ,结果表明 :HBSA CO1化合物是较好的解偶联剂 ,其解偶联活性高于N ( 2 ,4 ,5 三氯 )苯基 2 羟基 ( 3 ,5,6 三氯 )苯磺酰胺化合物和DNP .因此 ,根据其杀虫机理推测该化合物可能具有较好的杀虫活性 .The drug compound:N (2,5 dimethyl 4 benzoyl )phenyl 2 hydroxyl 3,5,6 trichlorobenzenesulfonamilide (HBSA CO1) was synthesized in this paper,and this compound was characterized by IR spectra, 1HNMR spectra as well as elemental analysis.By the methods of measuring respiratory activities using a clark oxygen electrode,measuring the change of inorganic phosphate in the respiratory process of mitochondria and measuring the adenosine triphosphatase activity,the drug′s uncoupling action of the oxidative phosphorylation in mitochondria was studied.The results showed that the title drug compound was a good uncoupler for the oxidative phosphorlation and its uncoupling activity was higher than the commercial drug compound N (2,4,5 trichloro)phenyl 2 hydroxyl 3,5,6 trichlorobenzenesulfonamilide(HBSN) for the parasite fasciola hepatica and typical uncoupler DNP.

关 键 词：HBSA-CO1 解偶联 杀虫活性 抗肝片吸虫病药物 

分 类 号：S859.795[农业科学—临床兽医学]