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新型 4-甲基伞形酮酰胺衍生物的合成、表征及生物活性。

Novel 4-Methylumbelliferone Amide Derivatives: Synthesis, Characterization and Pesticidal Activities.

机构信息

Research Center of Agro-Bionic Engineering & Technology of Shandong Province, College of Chemistry & Pharm., Qingdao Agricultural University, Qingdao 266109, China.

出版信息

Molecules. 2018 Jan 8;23(1):122. doi: 10.3390/molecules23010122.

DOI:10.3390/molecules23010122
PMID:29316710
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6017845/
Abstract

A series of novel 4-methylumbelliferone amide derivatives were designed, synthesized and characterized by ¹H NMR, C NMR and HR-ESI-MS. The structures of compounds and (compounds named by authors) were further confirmed by X-ray single crystal diffraction. The acaricidal, herbicidal and antifungal activities of the synthesized compounds were assayed for their potential use as pesticide. The results indicated that compounds , and were strong acaricidals against , with 72h corrected mortalities of greater than 80% at 1000 mg/L. Meanwhile, compounds and exhibit the strongest inhibition against the taproot development of and , and were even more potent than the commercial herbicide Acetochlor against . In addition, compounds , and showed the highest antifungal activity against the mycelium growth of , which makes them more effective than commercial fungicide Carbendazim.

摘要

设计、合成并通过 1H NMR、C NMR 和 HR-ESI-MS 对一系列新型 4-甲基伞形酮酰胺衍生物进行了表征。化合物 和 (作者命名的化合物)的结构通过 X 射线单晶衍射进一步得到证实。对合成化合物的杀螨、除草和抗真菌活性进行了测定,以期将其用作农药。结果表明,化合物 、 和 对 具有很强的杀螨活性,在 1000mg/L 时,72h 校正死亡率均大于 80%。同时,化合物 和 对 和 的主根发育表现出最强的抑制作用,甚至比商业除草剂乙草胺对 的抑制作用更强。此外,化合物 、 和 对 的菌丝生长表现出最高的抗真菌活性,比商业杀菌剂多菌灵更有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e110/6017845/24f4f2bfbd69/molecules-23-00122-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e110/6017845/097cb945bc3c/molecules-23-00122-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e110/6017845/24f4f2bfbd69/molecules-23-00122-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e110/6017845/097cb945bc3c/molecules-23-00122-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e110/6017845/24f4f2bfbd69/molecules-23-00122-g001.jpg

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