N-(1,4-二取代吡唑基)-1,2,3-噻二唑酰胺类化合物的抗植物病毒活性研究

Antivirus Activity of N-( 1,4-Substitued-Pyrazole-yl)-1,2,3-thiadiazole Carboxamide Derivatives

[目的]吡唑和噻唑类化合物是一类具有广泛生物活性的化合物,为了寻找到高活性的杂环酰胺类化合物,对此类化合物做进一步研究。[方法]对已合成的16个N-(1,4-取代吡唑基)-1,2,3-噻二唑酰胺类化合物分别进了抗烟草花叶病毒(TMV)和黄瓜花叶病毒(CMV)生物活性测试。[结果]初步生物活性表明,部分目标化合物在500μg/mL浓度下对烟草花叶病毒(TMV)和黄瓜花叶病毒(CMV)有一定的治疗活性,其中化合物TM-1在浓度为500μg/mL时,对TMV和CMV的治疗抑制率分别为41.75%和41.25%;化合物TM-13在浓度为500μg/mL时,对CMV的治疗抑制率分别为45.72%,比对照药剂宁南霉素58.72%略低,具有进一步研究的价值。

[ Aims ] Pyrazole and Thiazole derivates are very important compounds which exhibits high and broad- spectrum activity. In order to find heterocyclic carboxamide derivatives with high activity, and make further re- search about these compounds. [ Methods ] 16 synthesized N-（ 1,4 disubstituted pyrazole-yl） -1,2,3-thiadiazole carboxamide compounds were bioassayed against Tobacco mosaic virus （TMV） and Cucumber mosaic virus （CMV）. [ Results] The results indicats some of the synthesized compounds possessed antivirus activity to a cer- tain extent, among which compounds TM-1 displayed 41.75%和41.25% activities against TMV and CMV at 500 μg/mL, and TM-13 displayed 45.72% activities against CMV at 500μg,/mL. The molecule structures of the target compounds could be optimized based on the designed compounds.