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合成、表征、抗氧化活性及体内外抗菌评价的一些新偶氮苯甲酰胺和偶氮咪唑啉酮衍生物的急性毒性研究。

Synthesis, characterization, antioxidant power and acute toxicity of some new azo-benzamide and azo-imidazolone derivatives with in vivo and in vitro antimicrobial evaluation.

机构信息

Department of Chemistry, College of Education, Salahaddin University - Hawler, Erbil-Kurdistan, Iraq.

出版信息

Bioorg Chem. 2019 Apr;85:431-444. doi: 10.1016/j.bioorg.2019.01.014. Epub 2019 Jan 9.

DOI:10.1016/j.bioorg.2019.01.014
PMID:30685693
Abstract

In this research paper, a stepwise chemical reaction was conducted to synthesize and develop of a new potent azo-oxazolone, which was used as prototypical molecule for production of two series of azo-benzimide (5a-j) and azo-imidazolone (6a-j). FT-IR, H NMR, C NMR and CHN analysis were used for the structural elucidation. The high biological efficiency of newly obtained compounds was confirmed by in vitro antioxidant efficacy and in vitro antimicrobial activity against gram-positive and gram-negative bacteria via disc diffusion and tube dilution techniques. In addition, in vivo anti-microbial activity of some of the synthesized compounds was determined by using burnt rats which infected by Staphylococcus aureus. Tested compounds have shown high anti-microbial activity and wound healing in comparison to ucederm as a control. In vivo acute toxicity was carried out by up and down method for the compounds 4, 5d and 6d. The limited test dose was 2000 mg/kg, while the maximum tolerated dose was 5000 mg/kg which has administered no lethality recorded.

摘要

在这项研究论文中,进行了逐步的化学反应,以合成和开发一种新的有效的偶氮-噁唑啉,它被用作生产两个系列的偶氮-苯并咪唑(5a-j)和偶氮-咪唑啉(6a-j)的原型分子。傅里叶变换红外光谱(FT-IR)、核磁共振氢谱(H NMR)、核磁共振碳谱(C NMR)和元素分析(CHN)用于结构阐明。通过圆盘扩散和管稀释技术,体外抗氧化功效和体外抗革兰氏阳性和革兰氏阴性细菌的抗菌活性证实了新获得的化合物具有很高的生物效率。此外,通过烧伤大鼠感染金黄色葡萄球菌,测定了一些合成化合物的体内抗菌活性。与对照组的 ucederm 相比,测试化合物表现出高的抗菌活性和伤口愈合能力。通过上下法对化合物 4、5d 和 6d 进行了体内急性毒性试验。限定的测试剂量为 2000mg/kg,而最大耐受剂量为 5000mg/kg,没有记录到致死性。

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