Reaction of 6-alkoxy-2-oxo-2H-chromen-4-carbaldehydes with N-(2,3,4,6-tetra-O-acetyl-β-d-glucopyranosyl)thiosemicarbazide yielded corresponding thiosemicarbazones having 2H-chromen-2-one ring. In vitro evaluations showed that these 2H-chromen-2-one compounds exhibited remarkable antibacterial and antifungal activities against some typical bacteria and fungi. Representative compounds with MIC values of 0.78 − 1.56 μg/mL were 6c, 6g (against S. aureus), 6a, 6f (against S. epidermidis) (Gram-positive bacterial strains), 6e, 6g (against E. coli), 6b, 6e (against K. pneumoniae), and 6d–f (against S. typhimurium) (Gram-negative bacterial strains). Almost all thiosemicarbazones 6a–g had no activity against Gram-positive bacterial strain B. subtilis at these MIC values. Some compounds had strong inhibitory activity against several bacteria, such as 6b (for K. pneumoniae and S. typhimurium), 6d, 6e (for E. coli, K. pneumoniae, and S. typhimurium), 6f (for S. aureus, E. coli, and S. typhimurium), and 6g (for B. subtilis, S. aureus, E. coli, and K. pneumoniae). Some compounds had remarkable inhibitory activity against three clinical MRSA isolates with MIC values of 0.78–6.25 μg/mL. Docking study showed that compound 6g is compatible with the active site of S. aureus DNA gyrase 2XCT, which suggested that the tested compounds inhibited the synthesis of this enzyme.

的反应6-烷氧基-2-氧代-2- ħ -苯并吡喃-4- carbaldehydes与ñ - （2,3,4,6-四- ø -乙酰基β- d吡喃葡萄糖基），具有2氨基硫脲，得到相应的缩氨基硫脲ħ - chromen-2-one环。体外评估表明，这2 H -chromen-2-one化合物对某些典型的细菌和真菌显示出显着的抗菌和抗真菌活性。MIC值为0.78-1.56μg/ mL的代表性化合物为6c，6g（对抗金黄色葡萄球菌），6a，6f（对抗表皮葡萄球菌）（革兰氏阳性细菌菌株），6e，6g（针对大肠杆菌），6b，6e（针对肺炎克雷伯氏菌）和6d – f（针对鼠伤寒沙门氏菌）（革兰氏阴性细菌菌株）。在这些MIC值下，几乎所有的thiosemicarbazones 6a–g对革兰氏阳性细菌枯草芽孢杆菌均无活性。一些化合物对几种细菌具有很强的抑制活性，例如6b（对于肺炎克雷伯菌和鼠伤寒沙门氏菌），6d，6e（对于大肠杆菌，肺炎克雷伯氏菌和鼠伤寒沙门氏菌），6f（对于金黄色葡萄球菌，大肠杆菌和鼠伤寒沙门氏菌）和6g（对于枯草芽孢杆菌，金黄色葡萄球菌，大肠杆菌和肺炎克雷伯菌）。一些化合物对三种临床MRSA分离物具有显着的抑制活性，其MIC值为0.78–6.25μg/ mL。对接研究表明，化合物6g与金黄色葡萄球菌DNA促旋酶2XCT的活性位点兼容，这表明所测试的化合物抑制了该酶的合成。