新型含喹啉酮结构的三唑磺酰胺衍生物的合成及其对线粒体复合物Ⅲ的抑制活性

Synthesis and Biological Activities of Novel Triazolesulfonamide Derivatives Containing Quinolin-2-one Moiety

线粒体复合物Ⅲ是细胞呼吸链的重要组成部分,也是杀菌剂的重要作用靶标之一.根据生物电子等排、活性亚结构拼接原理,设计并合成了一系列含喹啉酮结构三唑磺酰胺衍生物,经质谱、氢谱、碳谱及元素分析对其结构进行了确认,测试了该类化合物对猪心线粒体复合物Ⅲ的抑制活性,结果表明目标化合物6f[IC_(50)=(45.75±1.02)μmol/L]对复合物Ⅲ的抑制活性较对照药剂吲唑磺菌胺[IC_(50)=(92.96±1.30)μmol/L]提高了一倍多,可作为先导结构进一步优化.

Complex Ⅲ is an essential component for cellular respiration chain and one of the most important targets of fungicides. According to bioisosterism and combination of bioactive sub-structive, a series of novel triazolesulfonamide derivatives containing quinolin-2-one moiety were designed and synthesized. The structures of the synthesized compounds were confirmed by MS, ^1H NMR, ^13 C NMR and elemental analysis. The antibacterial activities of these compounds against porcine complex Ⅲ were evaluated, and the bioassay results indicated that the target compound 6f [IC50=（45.75±1.02） μmol/L]showed much higher inhibitory potency（more than one-fold higher） against complex Ⅲ than that of the control amisulbrom [IC50=（92.96±1.30） μmol/L], thus compound 6f may recognize as a lead for further structure modification.