Synthesis of novel 1,3,4-oxadiazole derivatives containing diamides as promising antibacterial and antiviral agents
Synthesis of novel 1,3,4-oxadiazole derivatives containing diamides as promising antibacterial and antiviral agents
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含有二酰胺的新型 1,3,4-恶二唑衍生物的合成作为有前途的抗菌和抗病毒剂
DOI：
10.1007/s11164-017-2980-x
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发表时间：
2017-06
影响因子：
3.3
通讯作者：
Yang Song
中科院分区：
文献类型：
--
作者：
Wang Pei-Yi;Shao Wu-Bin;Xue Hai-Tao;Fang He-Shu;Zhou Jian;Wu Zhi-Bing;Song Bao-An;Yang Song
本文合成了一系列含二酰胺的1，3，4-恶二唑衍生物，并对其抗菌和抗病毒活性进行了研究。初步的抑菌活性测试表明，部分中间体和标题化合物对植物病原菌黄单胞菌的生长具有良好的抑制作用。（Xoo）和轴足黄单胞菌致病变种（Xanthomonaxonopodispv.）Citri（Xac）.进一步的研究表明，化合物H15对Xoo和Xac表现出最强的活性，最小EC 50值分别为0.7和5.9 μg/mL。抗病毒活性测定表明，这些结构中的一些显示出明显的治疗活性和中等的保护作用，对烟草花叶病毒（TMV）在体内。其中化合物H8对TMV的治疗效果最好，在500 μg/mL浓度下的治疗率为60.0%，与市售农用抗病毒剂宁南霉素的治疗率（54.2%）相当。该类化合物具有显著的生物活性，有望成为抗菌和抗病毒化疗研究的新先导化合物。
In this paper, a variety of novel 1,3,4-oxadiazole derivatives possessing diamides were synthesized and tested for their antibacterial and antiviral activity. Preliminary antibacterial assays indicated that some intermediates and title compounds displayed excellent inhibition effects against plant pathogens Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac). Further studies revealed that compound H15 exhibited the strongest activities against Xoo and Xac with minimal EC50 values of 0.7 and 5.9 μg/mL, respectively. Antiviral bioassays suggested that some of these structures displayed appreciable curative activities and moderate protective effects against tobacco mosaic virus (TMV) in vivo. Among them, compound H8 exerted the best chemotherapeutic effect against TMV with the curative rate of 60.0% at 500 µg/mL, which was comparable with those of commercial agricultural antiviral agent ningnanmycin (54.2%). Given their significant biological activities, this kind of compound could serve as new leading compounds in the study of antibacterial and antiviral chemotherapy.
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具有杀虫活性的潜在抗病毒剂（氢化）阿魏酸衍生物的合成及特性
影响因子：
--
作者：
Huang GY;Cui C;Wang ZP;Li YQ;Xiong LX;Wang LZ;Yu SJ;Li ZM;Zhao WG
通讯作者：
Zhao WG
影响因子：
7.3
作者：
Teng P;Huo D;Nimmagadda A;Wu J;She F;Su M;Lin X;Yan J;Cao A;Xi C;Hu Y;Cai J
通讯作者：
Cai J
影响因子：
2.1
作者：
Maftei, Catalin V.;Fodor, Elena;Neda, Ion
通讯作者：
Neda, Ion
影响因子：
4.9
作者：
Graham, JH;Gottwald, TR;Achor, DS
通讯作者：
Achor, DS
影响因子：
2.7
作者：
Li, Pei;Shi, Li;Song, Bao-An
通讯作者：
Song, Bao-An