2-(苯并异噻唑啉-3-酮-2-基)芳香酯类化合物的合成及生物活性

Synthesis and antibacterial activity of 2-(3-oxobenzo[d]isothiazol2(3H)-yl)ethyl benzoates

通过取代苯甲酸与N-羟乙基苯并异噻唑啉-3-酮反应,制备了6个未见文献报道的2-(苯并异噻唑啉-3-酮-2-基)芳香酯类化合物,其结构均经红外光谱、核磁共振氢谱、质谱及元素分析确认。采用比浊法测定了目标化合物对革兰氏阳性菌(枯草芽孢杆菌Bacillus subtilis、金黄色葡萄球菌Staphylococcus aureus、白色葡萄球菌Staphylococcus albus)及革兰氏阴性菌(大肠杆菌Escherichia coli、肺炎克雷伯菌Klebsiella pneumoniae及绿脓杆菌Pseudomonas aeruginosa)的抑菌能力。结果表明,绝大多数化合物对金黄色葡萄球菌和白色葡萄球菌表现出优良的生长抑制活性,其半数抑菌浓度(MIC50)约为4 mg/L。

Six novel 2- （ 3-oxobenzo [ d ] isothiazol-2 （3H） -yl ） ethyl benzoates were synthesized by condensation of 2- （2-hydroxyethyl） benzo[ d ~ isothiazol-3 （2H） -one with substituted benzoic acids. All compounds were characterized by IR, 1H NMR, ESI-MS and elemental analysis. The organisms used in the biological activity assay included gram-positive bacteria （Bacillus subtilis, Staphylococcus aureus, Staphylococcus albus ） and gram-negative bacteria （Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa）. The results showed that most of the compounds exhibit excellent inhibition activity against B. subtilis and S. aureus with MIC50 value about 4 mg/L.