Synthesis And Biological Activity Of Amide Derivatives Containing1,2,4-triazole And Piperazine

Triazole and piperazine derivatives are two most important kinds in the N-containing heterocyclic compounds. Triazole drugs are widely used as fungal antibiotics, anti-mycobacterial, anti-tumor and anti-cancer activities in clinics. However, piperazine derivatives have attracted many attentions since their broad spectrum of biological activities such as anti-depressant, anti-inflammatory, anti-tumor etc. Moreover, piperazine derivatives showed intrinsic water-solubility since both the two substitutes in1,4-position of piperazine rings are typically alkaline. Then1,2,4-triazole derivative was modified by introducing piperazine in it to increase its water-solubility and reinforce its bio-activities.Twenty-two novel derivatives (A1-A22) were designed and synthesized. The method was shown as Scheme1.All these twenty-two compounds have not been reported in literature. In attention, the structures of these compounds have been characterized by IR,1H NMR13C NMR ESI-MS(or HRMS). Meanwhile, the preliminary in vitro biological activity testing to Ee109, HepG2and MGC803Cells have been carried by MTT method. The results shown that the inhibition rate of these compounds are reached76.03%,68.25%and77.45%.