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Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
Journal of Saudi Chemical Society ( IF 5.8 ) Pub Date : 2019-11-11 , DOI: 10.1016/j.jscs.2019.10.002
Huai-He Zhu , Dan Zeng , Ming-Wei Wang , Pei-Yi Wang , Yuan-Yuan Wu , Li-Wei Liu , Song Yang

Plant microbial diseases caused global production constraints have become one of the most challenging events, thus urgently needing to be addressed nowadays. To efficiently promote the discovery of promising antimicrobial surrogates, a type of 1,3,4-oxadiazole thioethers owning naturally bioactive thiazolium patterns was designed and fabricated. Antibacterial screening results revealed that title compounds could significantly inhibit the growth of pathogens Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri. And the related antibacterial efficacy was elevated by approximately 386-, 16-, and 24-folds comparing those of mainly used commercial agents bismerthiazol and thiodiazole copper. In vivo experiment suggested that A9 could manage rice bacterial blight with the corresponding curative and protection efficiencies of 48.01% and 50.55% at 200 μg/mL. Moreover, SEM patterns and fluorescence spectra were performed to explore the possible antibacterial mechanism. Preliminary antifungal bioassays revealed that these molecules paraded broad-spectrum inhibition effects against three tested fungal strains. Considering the simple molecular skeleton and significant biological actions, title compounds can be further explored as potential antimicrobial surrogates for managing plant bacterial and fungal diseases.



中文翻译:

天然生物活性噻唑鎓盐和1,3,4-恶二唑片段在单一分子结构中的整合,可作为预期的抗菌替代物

造成全球生产限制的植物微生物疾病已成为最具挑战性的事件之一,因此现今迫切需要解决。为了有效地促进有前途的抗微生物替代物的发现,设计并制造了一种具有天然生物活性噻唑鎓样式的1,3,4-恶二唑硫醚。抗菌筛选结果表明,标题化合物可以显着抑制病原菌Xanthomonas oryzae pv的生长。水稻青枯Ralstonia solanacearum)和轴腐黄单胞菌(Xanthomonas axonopodis pv)柠檬。与主要使用的商业药物比美噻唑和噻二唑铜相比,相关的抗菌功效提高了约386倍,16倍和24倍。体内实验提示A 9在200μg/ mL的条件下,可以控制稻瘟病,相应的治愈和保护效率分别为48.01%和50.55%。此外,通过扫描电镜(SEM)和荧光光谱来研究可能的抗菌机理。初步的抗真菌生物测定结果表明,这些分子具有对抗三种测试真菌菌株的广谱抑制作用。考虑到简单的分子骨架和重要的生物学作用,可以进一步研究标题化合物作为控制植物细菌和真菌疾病的潜在抗菌替代物。

更新日期:2019-11-11
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