title: Design, Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives.
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. Compounds6b,6e,6g,6i,7band7cwere identified as the most active ones, and the EC50values of these active compounds were further tested. Compared to the commonly used fungicide Azoxystrobin (0.0884 µM), compounds6b(0.0544 µM) and6e(0.0823 µM) displayed improved activity againstBotrytis cinerea.
authors.affiliation: Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China. mzzhang@njau.edu.cn.
authors.forename: Ming-Zhi
authors.initials: MZ
authors.lastname: Zhang
authors.affiliation: Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China. 2014811023@njau.edu.cn.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China. 2014111011@njau.edu.cn.
authors.forename: Jia-Qun
authors.initials: JQ
authors.lastname: Wang
authors.affiliation: Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China. njzhangwh@126.com.
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Zhang
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020171:Botrytis / Q000187:drug effects*; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006868:Hydrolysis; D008745:Methylation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D003374:Coumarins
keywords: antifungal activity; coumarin; ring-opening reaction; strobilurin; synthesis