Novel eugenol bearing oxypropanolamines: Synthesis, characterization, antibacterial, antidiabetic, and anticholinergic potentials
作者:Hayriye Genç Bilgiçli、Ali Kestane、Parham Taslimi、Oguz Karabay、Arlinda Bytyqi-Damoni、Mustafa Zengin、İlhami Gulçin
DOI:10.1016/j.bioorg.2019.102931
日期:2019.7
eugenol bearing oxypropanolamine derivatives were also effective inhibitors against α-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase (AChE) enzymes with Ki values in the range of 0.80 ± 0.24-3.52 ± 1.01 µM for hCA I, 1.08 ± 0.15-3.64 ± 0.92 µM for hCA II, 5.18 ± 0.84-12.46 ± 2.08 µM for α-glycosidase, and 11.33 ± 2.83-32.81 ± 9.73 µM for AChE, respectively
已经以高收率和实用的方法合成了其中四个是新颖的五个氧丙醇胺衍生物。通过琼脂良好扩散法与市售药物进行比较,评估了鲍曼不动杆菌,铜绿假单胞菌,大肠杆菌和金黄色葡萄球菌菌株对合成物质的体外抗菌敏感性。大多数细菌是耐多药的。结论是这些化合物比参考药物有效得多。这些带有丁香酚的羟丙醇胺衍生物也是α-糖苷酶,胞质碳酸酐酶I和II亚型(hCA I和II)以及乙酰胆碱酯酶(AChE)酶的有效抑制剂,其Ki值在0.80±0.24-3.52±1.01 µM的范围内。 hCA I,hCA II为1.08±0.15-3.64±0.92 µM,5.18±0.84-12.46±2。