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

Abstract

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, 1H and 13C 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.

Na2S2O3 Catalyzed Three‐Component Synthesis and Anti‐Bacterial Activity of 3‐Methyl‐4‐(hetero)arylmethylene isoxazole‐5(4H)‐ones

“…As a continuation of the previous work, [31,32] herein, we report an effective and novel one-pot three-component synthesis of 3-methyl-4-(hetero) arylmethylene isoxazole-5(4H)ones in water employing a cheap and environmental-friendly Na 2 S 2 O 3 as a catalyst, and 16 compounds were synthesized with moderate to high yields. Furthermore, the antibacterial activities of the obtained isoxazolone derivatives were evaluated using rifampicin as a positive control.…”