Design,Ultrasonic-assisted Synthesis and Evaluation In vitro Antimicrobial Activity of Bis-isoxazole Derivatives Bearing Chloro-pyridinyl Group  

作　　者：FENG Fan LI Jing ZHANG Zhihui FU Jiaxu ZHANG Yumin GU Qiang 

机构地区：[1]College of Chemistry,Jilin University,Changchun,130012,P.R.China [2]Drilling and Exploitation Technology for Oil Shale,National-Local Joint Engineering Laboratory of In-situ Conversion,Changchun,130021,P.R.China

出　　处：《Chemical Research in Chinese Universities》2021年第3期668-673,共6页高等学校化学研究（英文版）

摘　　要：An ultrasonic-assisted synthesis of bis-isoxazole derivatives was developed.Eight 3-(6-chloropyridin-3-yl)-5-{[(3-arylisoxazol-5-yl)methoxy]methyl}isoxazoles were synthesized by 1,3-dipolar cycloaddition reaction between substituted isoxazolyl alkyne compounds and 6-chloro-N-hydroxynicotinimidoyl chloride.The structures of the synthesized compounds were confirmed by HRMS,FTIR,^(1)H and^(13)C NMR spectroscopy.Wherein,the antifungal and antibacterial activities of target compounds were tested.The synthesized compounds 6a and 6h exhibited better antifungal activity in comparison with the standard drug itraconazole.The minimum inhibitory concentrations(MICs)of both compound 6a and compound 6h were both 4µg/mL against Candida albicans ATCC 10231.

关 键 词：ULTRASONIC-ASSISTED Bis-isoxazole 1 3-Dipolar cycloaddition Antimicrobial activity 

分 类 号：O62[理学—有机化学]