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香豆素开环衍生物的设计、合成及抗真菌活性

Design, Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives.

作者信息

Zhang Ming-Zhi, Zhang Yu, Wang Jia-Qun, Zhang Wei-Hua

机构信息

Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China.

出版信息

Molecules. 2016 Oct 17;21(10):1387. doi: 10.3390/molecules21101387.

DOI:10.3390/molecules21101387
PMID:27763520
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6273309/
Abstract

Based on our initial design, we synthesized two series of coumarin ring-opening derivatives by the reactions of hydrolysis and methylation. Results of antifungal screening in vitro showed that the target compounds exhibited potent activity against the six common pathogenic fungi. Compounds , , , , and were identified as the most active ones, and the EC values of these active compounds were further tested. Compared to the commonly used fungicide Azoxystrobin (0.0884 µM), compounds (0.0544 µM) and (0.0823 µM) displayed improved activity against .

摘要

基于我们的初始设计,我们通过水解和甲基化反应合成了两个系列的香豆素开环衍生物。体外抗真菌筛选结果表明,目标化合物对六种常见致病真菌表现出强效活性。化合物、、、、和被确定为活性最强的化合物,并对这些活性化合物的EC值进行了进一步测试。与常用杀菌剂嘧菌酯(0.0884 µM)相比,化合物(0.0544 µM)和(0.0823 µM)对表现出更高的活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/fab51394adb2/molecules-21-01387-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/27b8ad6ebd1f/molecules-21-01387-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/d14647e4e09f/molecules-21-01387-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/5cb01b701892/molecules-21-01387-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/fab51394adb2/molecules-21-01387-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/27b8ad6ebd1f/molecules-21-01387-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/d14647e4e09f/molecules-21-01387-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/5cb01b701892/molecules-21-01387-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a58/6273309/fab51394adb2/molecules-21-01387-g003.jpg

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