Potent antibacterial agents: pyridinium-functionalized amphiphiles bearing 1,3,4-oxadiazole scaffolds
Potent antibacterial agents: pyridinium-functionalized amphiphiles bearing 1,3,4-oxadiazole scaffolds
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有效的抗菌剂：带有 1,3,4-恶二唑支架的吡啶鎓功能化两亲物
DOI：
10.1007/s11696-016-0021-7
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发表时间：
2017-06
期刊：
影响因子：
2.2
通讯作者：
Yang Song
中科院分区：
文献类型：
--
作者：
Wang Pei-Yi;Zhou Lei;Zhou Jian;Fang He-Shu;Wu Zhi-Bing;Xue Wei;Song Bao-An;Yang Song
通过对苯基取代基和烷基长度的调控和优化，得到了一系列对3种植物病原菌具有较强抗菌活性的吡啶功能化两亲化合物。苯环上取代基对活性的抑制作用研究表明，取代基不是影响活性的关键因素。相比之下，随着烷基链长度的增加，抗菌效果显著增强。其中6c、6 f、6 h、6 i、6 k、6l、6 n和6 q对3种病原菌均表现出明显的抑制活性，半数有效浓度（EC 50）在0.128-1.98 μg/mL之间。此外，对病原体黄单胞菌黄单胞菌致病型的最小EC 50值。黄单胞菌Xanthomonaxonopodispv.柠檬酸的最低浓度分别为0.128和0.403 μg/mL，比我们以前的结果降低了约4倍。这类两亲化合物合成简单，具有杀菌活性，有望成为植物细菌性病害的理想杀菌剂。
Through tuning and optimizing the phenyl substituents and alkyl length, a series of pyridinium-functionalized amphiphiles possessing potent antibacterial activity toward three types of plant pathogenic bacteria were obtained. Investigations on the inhibition effect of substituents on the phenyl ring towards the bioactivity suggested that the substitutional group was not the crucial factor for the bioactivity. In comparison, the antibacterial effects could be significantly enhanced with increasing the length of alkyl chains. Among these amphiphiles, 6c, 6f, 6h, 6i, 6k, 6l, 6n, and 6q exhibited remarkable inhibition activities against the three pathogenic bacteria with the half-maximal effective concentration (EC50) values within 0.128–1.98 µg/mL. Furthermore, the minimum EC50 values against the pathogens Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri could reach to 0.128 and 0.403 µg/mL, respectively, which were decreased about four times than those of our previous results. Given their simple synthesis and biocidal antibacterial activity, this kind of amphiphiles could be developed as promising bactericides against plant bacterial diseases.
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影响因子：
--
作者：
Jun-Die Hu;Peiyi Wang;Yuan Lin;Jidong Zhang;Mark D. Smith;P. Pellechia;Song Yang;B. Song;Qian Wang
通讯作者：
Jun-Die Hu;Peiyi Wang;Yuan Lin;Jidong Zhang;Mark D. Smith;P. Pellechia;Song Yang;B. Song;Qian Wang
影响因子：
4.1
作者：
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通讯作者：
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影响因子：
16.6
作者：
Sambhy, Varun;Peterson, Blake R.;Sen, Ayusman
通讯作者：
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影响因子：
7.3
作者：
Haldar, J;Kondaiah, P;Bhattacharya, S
通讯作者：
Bhattacharya, S
影响因子：
14
作者：
Mueller, Rainer;Eidt, Andreas;Schmalz, Gottfried
通讯作者：
Schmalz, Gottfried