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基于金属的酰胺衍生化合物具有抗菌和抗真菌活性。

Metal-based carboxamide-derived compounds endowed with antibacterial and antifungal activity.

机构信息

Institute of Chemical Sciences, Bahauddin Zakariya University , Multan , Pakistan .

出版信息

J Enzyme Inhib Med Chem. 2014 Aug;29(4):517-26. doi: 10.3109/14756366.2013.815178. Epub 2013 Aug 5.

DOI:10.3109/14756366.2013.815178
PMID:23914928
Abstract

A series of three bioactive thiourea (carboxamide) derivatives, N-(dipropylcarbamothioyl)-thiophene-2-carboxamide (L(1)), N-(dipropylcarbamothioyl)-5-methylthiophene-2-carboxamide (L(2)) and 5-bromo-N-(dipropylcarbamothioyl)furan-2-carboxamide (L(3)) and their cobalt(II), copper(II), nickel(II) and zinc(II) complexes (1)-(12) have been synthesized and characterized by their IR,(1)H-NMR spectroscopy, mass spectrometry and elemental analysis data. The Crystal structure of one of the ligand, N-(dipropylcarbamothioyl)thiophene-2-carboxamide (L(1)) and its nickel(II) and copper(II) complexes were determined from single crystal X-ray diffraction data. All the ligands and metal(II) complexes have been subjected to in vitro antibacterial and antifungal activity against six bacterial species (Escherichia coli. Shigella flexneri. Pseudomonas aeruginosa. Salmonella typhi. Staphylococcus aureus and Bacillus subtilis) and for antifungal activity against six fungal strains (Trichophyton longifusus. Candida albicans. Aspergillus flavus. Microsporum canis. Fusarium solani and Candida glabrata). The in vitro antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent than the parent ligands against one or more bacterial and fungal strains.

摘要

一系列三种生物活性硫脲(甲酰胺)衍生物,N-(二丙基碳酰硫代)噻吩-2-甲酰胺(L(1)),N-(二丙基碳酰硫代)-5-甲基噻吩-2-甲酰胺(L(2))和 5-溴-N-(二丙基碳酰硫代)呋喃-2-甲酰胺(L(3))及其钴(II),铜(II),镍(II)和锌(II)配合物(1)-(12)已通过其红外光谱,(1)H-NMR 光谱,质谱和元素分析数据进行了合成和表征。配体之一的晶体结构,N-(二丙基碳酰硫代)噻吩-2-甲酰胺(L(1))及其镍(II)和铜(II)配合物,是从单晶 X 射线衍射数据中确定的。所有配体和金属(II)配合物都进行了体外抗菌和抗真菌活性测试,以评估它们对六种细菌(大肠杆菌、福氏志贺菌、铜绿假单胞菌、伤寒沙门氏菌、金黄色葡萄球菌和枯草芽孢杆菌)和六种真菌(红色毛癣菌、白色念珠菌、黄曲霉、犬小孢子菌、腐皮镰刀菌和光滑念珠菌)的活性。体外抗菌和抗真菌生物活性数据表明,金属(II)配合物对一种或多种细菌和真菌菌株的活性比母体配体更强。

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