3,4-二芳基吡唑衍生物的合成与抑菌活性

Synthesis and Antibacterial Activities of 3,4-Diarylpyrazole Derivatives

以葛根素为起始原料,经烷基化反应得到7,4'-烃基取代葛根素衍生物,再由葛根素及其衍生物与水合肼"一锅法"直接制得6个3,4-二芳基吡唑衍生物,并对其合成条件进行了优化,用乙醇作溶剂,葛根素及其衍生物与水合肼在85℃下反应2 h,产率都超过70%。目标化合物的结构经IR、1HNMR、13CNMR和元素分析方法进行表征。初步生物活性测试表明,部分化合物表现出良好的抗菌活性,其中Ⅲa,Ⅲc,Ⅲf具有与氟康唑相近甚至更好的抑菌活性。

3,4-diarylpyrazole derivatives were synthesized from puerarin and its alkylated derivatives through one-pot reaction with hydrazine hydrate. The synthetic conditions of 3,4-diarylpyrazole derivatives were optimized,using ethanol as solvent,and with the reaction taking place at 85 ℃ for 2 h;the yield under such conditions was over 70%. The structures of these compounds were characterized by means of IR,1HNMR,13 CNMR spectra and elemental analysis. The fungicidal activities of these compounds were also evaluated. Most of them exhibit good activities. Compounds Ⅲ a,Ⅲ c,and Ⅲ f have similar or more evident antibacterial effects than that of fluconazole.