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Novel thymol bearing oxypropanolamine derivatives as potent some metabolic enzyme inhibitors – Their antidiabetic, anticholinergic and antibacterial potentials
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-08-07 , DOI: 10.1016/j.bioorg.2018.08.003
Mustafa Zengin , Hayriye Genc , Parham Taslimi , Ali Kestane , Ertugrul Guclu , Aziz Ogutlu , Oguz Karabay , İlhami Gulçin

A series of classical and newly synthesized thymol bearing oxypropanolamine compounds were synthesized and characterized. Their in vitro antibacterial activity on A. baumannii, P. aeruginosa, E. coli and S. aureus strains were investigated with agar well diffusion method. The results were compared with commercially available drug active compounds. As well as 3a, 3b and 3c have the most significant antibacterial effect among all the tested compounds; approximately all of them have more antibacterial activity than the reference drugs. These novel thymol bearing oxypropanolamine derivatives were effective inhibitors of the α-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase enzymes (AChE) with Ki values in the range of 463.85–851.05 µM for α-glycosidase, 1.11–17.34 µM for hCA I, 2.97–17.83 µM for hCA II, and 13.58–31.45 µM for AChE, respectively.



中文翻译:

新型百里酚带有氧丙醇胺衍生物,可作为某些代谢酶抑制剂的强效药物-具有抗糖尿病,抗胆碱能和抗菌的潜能

合成并表征了一系列经典的和新合成的带有氧丙醇胺化合物的百里酚。用琼脂微孔扩散法研究了它们对鲍曼不动杆菌,铜绿假单胞菌,大肠杆菌金黄色葡萄球菌的体外抗菌活性。将结果与可商购的药物活性化合物进行比较。以及3a3b3c在所有测试化合物中具有最显着的抗菌作用;几乎所有这些药物都比参考药物具有更大的抗菌活性。这些新型的带有百里酚的羟丙醇胺衍生物是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)的有效抑制剂,其α-的K i值范围为463.85-851.05 µM。糖苷酶,hCA I为1.11–17.34 µM,hCA II为2.97–17.83 µM,AChE为13.58–31.45 µM。

更新日期:2018-08-07
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