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Synthesis, Structures, and Interactions with CT-DNA/BSA of Three New Acylhydrazones Containing Oxazole Ring
Heterocycles ( IF 0.6 ) Pub Date : 2020-11-13 , DOI: 10.3987/com-20-14355
Xiangrong Liu , Lingling Chang , Zaiwen Yang , Shunsheng Zhao , Xinjuan Chen , Bosen Dai

Three new acylhydrazones containing oxazole ring C11H8N3O2X (X = F, 1; Br, 2; I, 3) have been synthesized. The single crystal XRD presented that 1 belonged to the monoclinic system, while 2 and 3 belonged to the triclinic systems. TG-DTG results showed that the maximum thermal decomposition temperatures of 1-3 were more than 260 °C. The UV-vis spectra, fluorescence spectra and microcalorimetry measurements indicated that each acylhydrazone bound to calf thymus DNA (CT-DNA) via groove binding mode and interacted with bovine serum albumin (BSA) by static quenching effect and the corresponding interaction processes were all exothermic. The molecular docking showed that each acylhydrazone bound to CT-DNA and BSA mainly through hydrogen bonding. The minimum inhibitory concentrations of 1-3 against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, and Pseudomonas aeruginosa were all about 0.25 mg·mL-1.

中文翻译:

三种新型含恶唑环的酰基hydr的合成,结构及与CT-DNA / BSA的相互作用

合成了三个新的含恶唑环C 11 H 8 N 3 O 2 X(X = F,1 ; Br,2 ; I,3 )的酰基hydr 单晶XRD表明1属于单斜晶系,而23属于三斜晶系。TG-DTG结果表明,最大热分解温度1 - 3分别超过260℃。紫外可见光谱,荧光光谱和微量热法测量表明,每个都通过小牛胸腺DNA(CT-DNA)结合并以静态猝灭作用与牛血清白蛋白(BSA)相互作用,并发生相应的相互作用过程。分子对接表明每个酰基hydr主要通过氢键与CT-DNA和BSA结合。的最低抑菌浓度1 - 3大肠杆菌金黄色葡萄球菌枯草芽孢杆菌,和铜绿假单胞菌均约0.25mg·ML -1
更新日期:2020-11-13
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