Effective Synthesis and Anti-Mycobacterial Activity of Isoxazole-Substituted Piperazine Derivatives

Graphical 1,4-Bis((3-arylisoxazol-5-yl)methyl)piperazines were synthesized in 64–90 % yield by an environment friendly method using 5-(bromomethyl)-3-arylisoxazoles and piperazine as raw materials. Their antibacterial activities were evaluated. A series of piperazine derivatives containing bis-isoxazole were successfully synthesized by the reaction between piperazine and substituted isoxazole derivatives under the optimal reaction condition. The structures of all products were confirmed by IR, HRMS, 1 H and 13 C NMR. The antibacterial activities of all products against Mycobacteria smegmatis in vitro were tested using rifampin as a positive control. Two compounds presented wonderful anti-mycobacterium activity, and their minimum inhibitory concentrations were respectively 2.60±1.11 μmol/mL and 4.35±0.00 μmol/mL, which indicated that they can be regarded as candidates for development of anti-TB drugs.