Synthesis and bioactivities of 1-aryl-4-hydroxy-1H-pyrrol-2(5H)-one derivatives bearing 1,3,4-oxadiazole moiety
Synthesis and bioactivities of 1-aryl-4-hydroxy-1H-pyrrol-2(5H)-one derivatives bearing 1,3,4-oxadiazole moiety
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带有1,3,4-恶二唑部分的1-芳基-4-羟基-1H-吡咯-2(5H)-酮衍生物的合成和生物活性
DOI：
10.1016/j.jscs.2016.10.002
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发表时间：
2017-03-01
影响因子：
5.6
通讯作者：
Yang, Song
中科院分区：
文献类型：
--
作者：
Wang, Pei-Yi;Chen, Ling;Yang, Song
本文设计合成了含1，3，4-恶二唑基的1-芳基-4-羟基-1H-吡咯基-2(5H)-酮类化合物。初步的生物活性测试表明，这些化合物不仅对包括水稻白叶枯病菌在内的植物病原菌表现出良好的抑菌活性。Oryzae(Xoo)、青枯病菌Ralstonia solanacearum(R.solanacearum)和轴突黄单胞菌Xanthomonas axonopodis PV.西特里。(XAc)，但对烟草花叶病毒(TMV)也有一定的治疗和保护作用。进一步的研究表明，化合物8a和8l对Xoo的抑制效果最好，其半最大有效浓度(EC50)分别为8.6和7.3mU g/m L，优于商品化农用抗菌剂双硫唑(EC50=92.6 m g/m L)。鉴于上述结果，这类化合物可以作为替代抗菌剂进行进一步的研究和开发。(C)2016年沙特国王大学。爱思唯尔B.V.制作和主办。
In this paper, a variety of 1-aryl-4-hydroxy-1H-pyrrol-2(5H)-one derivatives bearing 1,3,4-oxadiazole moiety were designed and synthesized. Preliminary bioassays suggested that these compounds not only exhibited favorable antibacterial activity toward plant pathogenic bacteria including Xanthomonas oryzae pv. oryzae (Xoo), Ralstonia solanacearum (R. solanacearum), and Xanthomonas axonopodis pv. citri. (Xac), but also demonstrated certain curative and protective activities against Tobacco mosaic virus (TMV). Further studies revealed that compounds 8a and 8l exerted the best inhibition effect against Xoo with the half-maximal effective concentration (EC50) values of 8.6 and 7.3 mu g/mL, respectively, which were better than that of commercial agricultural antibacterial bismerthiazol (EC50 = 92.6 mu g/mL). Given the above results, this kind of compounds can be further studied and explored as alternative antibacterial agents. (C) 2016 King Saud University. Production and hosting by Elsevier B.V.