Synthesis and Antifungal Activity of Novel Myrtenal-Based 4-Methyl-1,2,4-triazole-thioethers.
Synthesis and Antifungal Activity of Novel Myrtenal-Based 4-Methyl-1,2,4-triazole-thioethers.
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新型桃金娘醛基4-甲基-1,2,4-三唑硫醚的合成及其抗真菌活性
DOI：
10.3390/molecules22020193
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发表时间：
2017-01-24
期刊：
影响因子：
--
通讯作者：
Lei FH
中科院分区：
文献类型：
--
作者：
Lin GS;Duan WG;Yang LX;Huang M;Lei FH
通过多步反应，设计合成了一系列含1，2，4-三氮唑环的桃金娘烯醛类化合物，以期开发出高效的抗真菌药物。其结构经UV-Vis、FTIR、核磁共振、电喷雾质谱确证。采用体外抗枯萎病菌活性的方法初步评价了目标化合物的抗真菌活性。黄瓜、轮纹疫霉菌、茄链格孢菌、花生尾孢霉和玉米赤霉菌的最低抑菌浓度为50微克/毫升。化合物6c(R=i-Pr)、6l(R=o-NO2 Bn)和6a(R=Et)对螺旋藻的抑菌率分别为98.2%、96.4%和90.7%，与市售杀菌剂嘧菌酯相当或更强，抑制率为96.0%。
A series of novel myrtenal derivatives bearing 1,2,4-triazole moiety were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Their structures were confirmed by using UV-vis, FTIR, NMR, and ESI-MS analysis. Antifungal activity of the target compounds was preliminarily evaluated by the in vitro method against Fusarium oxysporum f. sp. cucumerinum, Physalospora piricola, Alternaria solani, Cercospora arachidicola, and Gibberella zeae at 50 µg/mL. Compounds 6c (R = i-Pr), 6l (R = o-NO2 Bn), and 6a (R = Et) exhibited excellent antifungal activity against P. piricola with inhibition rates of 98.2%, 96.4%, and 90.7%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide azoxystrobin with a 96.0% inhibition rate, which served as a positive control.
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