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为研究新型吡唑类杂环衍生物的生物活性,从5-烷基-1H-吡唑-3-甲酸乙酯(1)出发,设计合成了18个具有双杂环结构的N-(取代-1H-吡唑-4-基)-1H-吡唑-3(5)-甲酰胺类化合物,目标化合物的结构均经过核磁共振氢谱(1H NMR)和高分辨质谱(HRMS)确证,并通过X射线衍射法解析了目标物10b的单晶结构.生物活性测试表明:(i)大部分目标化合物具有较好抗烟草花叶病毒活性,其中化合物10b和10l的活性高于同浓度的对照药剂宁南霉素(Ningnanmycin)及病毒唑(Virazole);(ii)所有目标物对粘虫(Mythimna separata)和蚊幼虫(Culex pipiens pallens)具有一定的杀灭作用,但活性普遍不高,600×10-6 g/m L浓度下,10d对粘虫的杀灭活性为40%,5×10-6 g/m L浓度下,10f和10k对蚊的幼虫的杀灭活性达70%;(iii)50×10-6 g/m L浓度下,除10h对芦笋茎枯菌(Phoma asparagi Sacc.)有64%的抑制率,10q对棉花立枯菌(Rhizoctonia solani)有50%的抑制率外,其余化合物无明显杀菌活性.上述结果表明,此类化合物可作为杀虫剂或抗植物病毒剂先导做进一步深入研究.
In order to study the biological activity of novel pyrazole heterocyclic derivatives, 18 N- (substituted ones with double heterocyclic structure) were designed and synthesized from 5-alkyl-1H-pyrazole-3-carboxylic acid ethyl ester Pyrazole-3-yl) -1H-pyrazole-3 (5) -carboxamides. The structures of the target compounds were confirmed by 1H NMR and HRMS. The single crystal structure of target 10b was analyzed by X-ray diffractometry.The biological activity tests showed that: (i) most of the target compounds had better anti-tobacco mosaic virus activity, of which compounds 10b and 101 were higher than the same concentration Ningnanmycin and Virazole; (ii) All the targets have some killing effect on Mythimna separata and Culex pipiens pallens, but the activity is generally not high. 600 The killing activity of 10f and 10k against mosquito larvae was 70% under the concentration of 10-6 g / ml for 10 days. (iii) 50% inhibition of 10q against Rhizoctonia solani at a concentration of 50 × 10-6 g / mL, with a 64% inhibition of Phoma asparagi Sacc. Rate, the remaining compounds without Obvious bactericidal activity.The above results show that these compounds can be further studied as a precursor of insecticide or anti-plant virus agent.