Synthesis and Antifungal Activity of 8-Substituded Coumarins
Twenty-three kinds of 8-substituded coumarins were synthesized by Perkin reaction and Knoevenagel reaction from 2-hydroxy-3-substituted benzaldehyde in yields of 66.2%-97.6%.The structures of the title compounds were characterized by FT-IR, 1H NMR, MS and elemental analysis.Their antifungal activities against mycelium growth of Botrytis cinerea, Citrusanthrax bacteria, Fusarium oxysporium and Valsa mali were measured.The results indicated that most of these compounds exhibited moderate to high antifungal activity.8-isopropyl coumarin showed strong fungi inhibition with EC50 of 21.74 and 27.14 mg/L against V.mall and C.bacteria respectively.The structure-activity relationship (SAR) showed that antifungal activity was enhanced when alkyl, aryl or halogen was introduced to C-8 of coumarin, while carboxylate, acetyl or phenyl on C-3 was detrimental to the antifungal activity.
coumarin synthesis antifungal activity
Wang Dong Wei Yan Zhang Xiangfei Hao Shuanghong
College of Chemistry & Pharm,Research Center of Agro-bionic Engineering & Tech.of Shandong Province,Qingdao Agricultural University,Qingdao Shandong 266109
国内会议
第十四届全国农药学科教育科研研讨会暨赵善欢学术思想与研究实践讨论会
广州
英文
82-89
2014-08-03（万方平台首次上网日期，不代表论文的发表时间）