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

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.