Synthesis, Biological Activities and Structure-Activity Relationships for New Avermectin Analogues
In an effort to discover new molecules with good insecticidal activities, more than 40 new avermectin derivatives were synthesized and their biological activities were determined against Tetranychus Cinnabarinus, Aphis craccivora and Bursaphelenchus xylophilus.Preliminary bioassays showed that most of the target compounds possessed good-to-excellent activities against three insect species.Notably, the majority of the target compounds exhibited high selectivity against T.cinnabarinus, some of which were much better in comparison with the commercial avermectin.Especially compounds 9j (LC50:0.005 μM) and 16d (LC50: 0.002aM) were 2.5-and 4.7-fold as high as the activity of avermectin (LC50:0.0131M), respectively, against T.cinnabarinus.Moreover, compounds 9b, 9d-f, 9h, 9j, 9I, 9n, 9p, 9r, 9v and 17d showed superior activities with LC50 values of 2.959-5.013 μM compared to that of 1 (LC50: 6.746 μM) against B.xylophilus.Meanwhile, the insecticidal activities of compounds 9f, 9g, 9h, and 9m against A.craccivora were 7~8 times better than that of avermectin, with LC50 values of 7.744, 5.634, 6.809, 7.939 and 52.234 μM, respectively.Furthermore, QSAR analysis showed that the molecular shape, size, connectivity degree and electronic distribution of avermectin analogues had substantial effects on insecticidal potency.These preliminary results provided useful insight in guiding further modifications of avermectin in the development of potential new insecticides.
Avermectin derivatives synthesis biological activity SAR analysis
Xiang Nan Hai-Tao Yu Yan Zhang Ying-Qian Liu Shao-Yong Zhang Guan-Fang Hu Huan-Xiang Liu An-Liang Chen Dan Wu
School of Pharmacy,Lanzhou University,Lanzhou 730000,PR China Institute of Plant Protection,Gansu Academy of Agricultural Sciences,Lanzhou730070,China Provincial Engineering Laboratory of Biopesticide Preparation,Zhejiang A&F University,Lin”an 311300,
国内会议
第十四届全国农药学科教育科研研讨会暨赵善欢学术思想与研究实践讨论会
广州
英文
100-114
2014-08-03（万方平台首次上网日期，不代表论文的发表时间）