为创制具有较高生物活性的绿色农药,以姜黄素为先导,将具有良好生物活性的肟酯基团引入1,4-戊二烯-3-酮的骨架中,设计合成了一系列含杂环1,4-戊二烯-3-酮肟酯类化合物,其结构经红外光谱、核磁共振氢谱及碳谱和高分辨质谱确认.初步的生物活性测试结果表明,在药剂浓度为50 mg/L时,化合物5d对小麦赤霉病菌,水稻纹枯病菌和苹果腐烂病菌的抑制活性相对较好,分别为64.75％、52.05％和69.68％;在药剂浓度为500 mg/L时,化合物5d、5e和5f对TMV具有较好的治疗和钝化活性,其抑制率分别为56.93％和86.89％、53.08％和83.51％、53.40％和89.01％.以上研究结果表明,1,4-戊二烯-3-酮肟酯类化合物具有一定抑菌和抗病毒活性,在其结构基础上进行适当的改造,有望获得具有较高生物活性的有机分子.
In order to explore novel green pesticide with potent biological activities,a series of novel 1,4-pentadien-3-one oxime ester derivatives bearing heterocycle moiety,derived from curcumin,was designed and synthesized.Their structures were confirmed by infrared spectroscopy,proton nuclear magnetic resonance spectroscopy(1H NMR),13C NMR,and high resolution mass spectroscopy(HRMS).The bioassays indicate that inhibition rates of compound 5d against G.zeae,F.ox-ysporum and C.mandshurica at 50 mg/L are 64.75％,52.05％ and 69.68％,respectively,and compounds 5d,5e and 5f have good curative and deactivation activities against tobacco mosaic virus at 500 mg/L,with the inhibition rates of 56.93％ and 86.89％,53.08％ and 83.51％,and 53.40％ and 89.01％,respectively.These indicate that 1,4-pentadien-3-one oxime ester is a valuable scafford to develope new compounds poessessing high biological activities such as potential antifungal and antiviral activities.
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