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来源于染料木黄酮的脱氧安息香衍生物的合成、晶体结构及抗菌活性

Synthesis, crystal structure and antimicrobial activity of deoxybenzoin derivatives from genistein.

作者信息

Li Huan-Qiu, Xue Jia-Yu, Shi Lei, Gui Shan-Ying, Zhu Hai-Liang

机构信息

Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.

出版信息

Eur J Med Chem. 2008 Mar;43(3):662-7. doi: 10.1016/j.ejmech.2007.05.013. Epub 2007 Jun 8.

Abstract

A series of deoxybenzoin derivatives from genistein were synthesized and their structures were elucidated by (1)H NMR, mass spectral data and micro analyses. The structures of 2, 7 and 10 were determined by single-crystal X-ray analysis. These obtained compounds were evaluated for their assayed antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus) and antifungal (Aspergillus niger, Candida albicans and Trichophyton rubrum) activities by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. Most compounds have displayed comparable antibacterial activity against bacterial. On the basis of the biological results, structure-activity relationships are discussed.

摘要

合成了一系列来自染料木黄酮的脱氧苯偶姻衍生物,并通过¹H NMR、质谱数据和微量分析对其结构进行了阐明。2、7和10的结构通过单晶X射线分析确定。通过MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐)法对这些所得化合物进行了抗菌(枯草芽孢杆菌、大肠杆菌、荧光假单胞菌和金黄色葡萄球菌)和抗真菌(黑曲霉、白色念珠菌和红色毛癣菌)活性测定。大多数化合物对细菌显示出相当的抗菌活性。基于生物学结果,讨论了构效关系。

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