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合成新型（E）-2-（4-（1H-1,2,4-三唑-1-基）亚乙烯基）-4-（烷基/芳基亚甲氧基）喹唑啉衍生物作为抗菌剂。

Synthesis of novel (E)-2-(4-(1H-1,2,4-triazol-1-yl)styryl)-4- (alkyl/arylmethyleneoxy)quinazoline derivatives as antimicrobial agents.

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Centre for Research and Development of Fine Chemicals, Guizhou University, Guiyang, 550025, China.

出版信息

Mol Divers. 2018 Feb;22(1):71-82. doi: 10.1007/s11030-017-9792-1. Epub 2017 Nov 8.

DOI:10.1007/s11030-017-9792-1
PMID:29119421
Abstract

A series of novel (E)-2-(4-(1H-1,2,4-triazol-1-yl)styryl)-4-(alkyl/arylmethyleneoxy)quinazoline derivatives (4a-4s) were synthesized in good to excellent yields, and their structures were fully characterized by [Formula: see text] NMR, [Formula: see text] NMR, HRMS and IR spectra. The structure of compound 4b was further confirmed via single-crystal X-ray diffraction analysis. The bioassay results indicated that compounds 4s, 4q and 4n inhibit phytopathogenic bacterium Xanthomonas axonopodis pv. citri (Xac) more potently than commercial bactericide bismerthiazol. However, not a single compound can effectively inhibit three pathogenic fungi tested at 50 [Formula: see text].

摘要

一系列新型（E）-2-（4-（1H-1,2,4-三唑-1-基）亚乙烯基）-4-（烷基/芳基亚甲基氧基）喹唑啉衍生物（4a-4s）以良好到优异的产率合成，其结构通过[Formula: see text]NMR、[Formula: see text]NMR、HRMS 和 IR 光谱进行了充分表征。通过单晶 X 射线衍射分析进一步确证了化合物 4b 的结构。生物测定结果表明，化合物 4s、4q 和 4n 对植物病原菌柑橘溃疡病菌（Xac）的抑制作用比商业杀菌剂双噻菌胺更强。然而，没有一种化合物在 50 [Formula: see text]下能有效抑制三种测试的致病真菌。

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