新型抗肝片吸虫病药物的合成及构效研究  

Synthesis and Structure-Activity Study of a New Kind of Fasciolicide

作　　者：李哲 沈俊菊[2] 赵军[2] 王晓晶[2] 新民[2] 

机构地区：[1]内蒙古兽药监察所 [2]内蒙古大学化学系

出　　处：《内蒙古石油化工》2002年第1期11-13,共3页Inner Mongolia Petrochemical Industry

基　　金：国家自然科学基金资助

摘　　要：本论文总结了我们课题组以前研究工作中的规律和经验 ,合成了 1 3个新型抗肝片吸虫病药物化合物。对化合物的高效液相色谱、红外、紫光及核磁共振氢谱物理性质、结构特征进行了表征 ,同时还做了生物活性的测试。综合几项测试指标 ,分析了药物化合物的物理性质、结构特征对其药效的影响。结果表明 :适宜的弱酸性 ( pka=3.6～ 6.0 )According to some guide ideas deriving from our previous studies, a series of fasciolicides were synthesized. We studied their physical properties?Structural features and uncoupling activities through HPLC?IR spectra?the electronic absorption spectra? 1-HNMR spectra and biological experiments. Experimental results indicated that moderate weak acidity (pk a=3.6～6.0) and hydrophobicity are essential for drug to possess potent fasciolicidal activity. We have screened some drugs with potent uncoupling activity such as 1 #?2 #?3 #?5 # and9 # in laboratory. Further pharmacodynamical research of these compounds should be made in future.

关 键 词：新型 抗肝片吸虫病药物 合成 构效 研究 解偶联作用 脂溶性 

分 类 号：TQ463[化学工程—制药化工] R978.6[医药卫生—药品]