Studies on Crude Drugs Effective on Visceral Larva Migrans. Part XVI. Nematocidal Activity of Long Alkyl Chain Amides, Amines, and Their Derivatives on Dog Roundworm Larvae.
作者:Fumiyuki KIUCHI、Satomi NISHZAWA、Hiromi KAWANISHI、Sayuri KINOSHITA、Hisanao OHSIMA、Akiyo UCHITANI、Noriko SEKINO、Miki ISHIDA、Kaoru KONDO、Yoshisuke TSUDA
DOI:10.1248/cpb.40.3234
日期:——
activity of amides and amines having a long alkyl chain against the second-stage larva of dog roundworm, Toxocara canis, was examined. Long chain acyl amides with smaller substituents on the nitrogen showed stronger activity and the activity of cyclic amine amides was stronger than that of acyclic ones. In a series of homologous amides, the activity was dependent on the alkyl chain length: it reached
检查了具有长烷基链的酰胺和胺对犬round虫第二阶段幼虫的杀线虫活性。在氮上具有较小取代基的长链酰基酰胺显示出更强的活性,环状胺酰胺的活性强于无环酰胺。在一系列同源酰胺中,活性取决于烷基链长:在最佳链长处达到最大值,而在较短和较长的同系物中均降低。通过使用双线性模型分析了同系物的活性与疏水性之间的关系。对于所有中性酰胺,提供最大活性的化合物的疏水性均相似,但分子中具有额外胺基的酰胺具有不同的值。具有长烷基链的叔胺及其盐也具有与相应酰胺相当的杀线虫活性。这些盐以低于其临界胶束浓度的浓度杀死幼虫,表明它们表现为杀线虫作用的单个分子。