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新型砜基哌啶酮衍生物的设计、合成与构效关系研究 作为潜在的抗真菌剂。

Design, Synthesis and Structure-Activity Relationship of Novel Pinacolone Sulfonamide Derivatives against as Potent Antifungal Agents.

机构信息

Department of Pesticide Science, Plant Protection College, Shenyang Agricultural University, Shenyang 110866, China.

出版信息

Molecules. 2022 Aug 25;27(17):5468. doi: 10.3390/molecules27175468.

DOI:10.3390/molecules27175468
PMID:36080238
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9458130/
Abstract

To develop new fungicides with high efficiency, 46 novel sulfonamide derivatives were designed and synthesized by introducing pinacolone fragment into chesulfamide which was used as lead compound. All compounds were characterized by H NMR, C NMR, and MS spectra, and the structure of compound was also confirmed by X-ray single crystal diffraction. It was found that a variety of compounds present excellent inhibitory effect against . The inhibition rates of on tomato and strawberry were 90.24% (200 mg/L) and 100% (400 mg/L) respectively, which were better than the lead compound chesulfamide (59.23% on tomato seedlings and 29.63% on strawberries).

摘要

为了开发高效的新型杀菌剂,我们通过在先导化合物 chesulfamide 中引入苍术酮片段,设计并合成了 46 种新型磺胺衍生物。所有化合物均通过 1H NMR、13C NMR 和 MS 谱进行了表征,化合物 的结构还通过 X 射线单晶衍射进行了确认。研究发现,多种化合物对 具有优异的抑制作用。化合物 对番茄和草莓的抑制率分别为 90.24%(200mg/L)和 100%(400mg/L),优于先导化合物 chesulfamide(对番茄幼苗的抑制率为 59.23%,对草莓的抑制率为 29.63%)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/4bfd77e326c2/molecules-27-05468-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d2dbe2eb8e24/molecules-27-05468-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d2b78a7fb70e/molecules-27-05468-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/8743d71fb12d/molecules-27-05468-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d49c224b5e2d/molecules-27-05468-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/ddc53cac0fe2/molecules-27-05468-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/6f4999c59a4f/molecules-27-05468-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/4bfd77e326c2/molecules-27-05468-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d2dbe2eb8e24/molecules-27-05468-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d2b78a7fb70e/molecules-27-05468-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/8743d71fb12d/molecules-27-05468-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/d49c224b5e2d/molecules-27-05468-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/ddc53cac0fe2/molecules-27-05468-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/6f4999c59a4f/molecules-27-05468-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/493f/9458130/4bfd77e326c2/molecules-27-05468-g006.jpg

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