Sakarya University, Science and Arts Faculty Chemistry Department, 54187-Serdivan Sakarya, Turkey.
Sakarya University, Science and Arts Faculty Chemistry Department, 54187-Serdivan Sakarya, Turkey.
Bioorg Chem. 2019 Jul;88:102931. doi: 10.1016/j.bioorg.2019.102931. Epub 2019 Apr 16.
Five oxypropanol amine derivatives that four of them are novel have been synthesized with high yields and practical methods. in vitro antibacterial susceptibility of Acinetobacter baumannii, Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus strains to synthesized substances were evaluated with agar well-diffusion method by comparison with commercially available drugs. Most of the bacteria were multidrug resistant. It was concluded that these compounds are much more effective than reference drugs. These 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 K 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.
已经用高产率和实用方法合成了五个羟丙基胺衍生物,其中四个是新的。通过琼脂孔扩散法与市售药物进行比较,评估了这些合成物质对鲍曼不动杆菌、铜绿假单胞菌、大肠杆菌和金黄色葡萄球菌菌株的体外抗菌敏感性。大多数细菌都是多药耐药的。结论是这些化合物比参考药物更有效。这些含有丁香酚的羟丙基胺衍生物也是α-糖苷酶、胞质碳酸酐酶 I 和 II 同工酶(hCA I 和 II)以及乙酰胆碱酯酶(AChE)的有效抑制剂,其 K 值范围分别为 0.80 ± 0.24-3.52 ± 1.01 µM 用于 hCA I、1.08 ± 0.15-3.64 ± 0.92 µM 用于 hCA II、5.18 ± 0.84-12.46 ± 2.08 µM 用于α-糖苷酶和 11.33 ± 2.83-32.81 ± 9.73 µM 用于 AChE。