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以天然存在的茵陈二炔(Capillene)为先导化合物,仿生合成了9个共轭二 块和3个单炔共12个化合物。经生物活性测定表明:合成的聚乙炔类化合物对仓库害 虫具有一定的毒杀、抑制繁殖和行为控制作用.其中化合物2、5、9、10试验剂量为 0.05%(w/w)时,能完全抑制米象(Sitophilus oryzae)的繁殖;化合物 2、5、8、9、10对锯 谷盗(Oryzaophilus Surinamensis)繁殖抑制率都在80%以上.对赤拟谷盗(Tribolium castaneum)抑制率在 80%以上的有 2、3、4、5、10几种;化合物 2、5、10对米象 致死中浓度(LC_(50))值分别为 0. 0128%,0. 0295%和 0.0069%;处理 96h后, 化合物5、6对赤拟谷盗成虫的忌避率分别为97.44%和91.89%;生化酶抑 制测定表明,化合物10对乙酸胆碱脂酶具有明显的抑制作用,其它几种化 合物的毒杀机理有待进一步研究。
A total of 12 compounds with 9 conjugated two and three monoalkyne were synthesized by using naturally occurring capillene as the lead compound. The results of bioassay showed that the synthesized polyacetylene compounds have some toxic effects on the storage pests and inhibit the reproduction and behavior control. Compounds 2, 5, 9 and 10 were able to completely inhibit the growth of Sitophilus oryzae when the test dose was 0.05% (w / w). Compounds 2, 5, 8, Oryzaophilus Surinamensis) reproduction inhibition rates are above 80%. The inhibitory rates of Tribolium castaneum were more than 80%, including 2, 3, 4, 5, and 10; the lethal concentrations of compounds 2, 5 and 10 (LC_ (50) 0. 0128%, 0. 0295% and 0.0069%, respectively. After treated for 96h, the repellent rates of compounds 5 and 6 on adults were 97.44% and 91.89%, respectively. The results of biochemical enzyme inhibition assay showed that the inhibition rates of compound 10 to acetic acid choline ester Enzyme has a significant inhibitory effect, the poisoning mechanism of several other compounds to be further studied.