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Synthesis and structures of 5-nitro-salicylaldehyde thiosemicarb-azonates of copper(II): molecular spectroscopy, ESI-mass studies, antimicrobial activity and cytotoxicity

机译:铜(II)的5-硝基-水杨醛醛硫代半氨基甲酸酯的合成及结构:分子光谱,ESI质谱研究,抗菌活性和细胞毒性

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The basic objective of this investigation is to explore potential metallo-organic antimicrobial agents based on metal-thiosemicarbazonates. This study acquires significance in the light of the antibacterial resistance exhibited by Gram-positive and Gram-negative bacteria which have become a serious global medical problem. The increasing drug resistant bacteria are responsible for various nosocomial infections and among these, methicillin resistant Staphylococcus aureus (MRSA) is the most frequent nosocomial pathogen. Likewise, Candida albicans (fungi) are found to have developed resistance against a number of antifungal agents. In this context, compounds of copper(II) with salicylaldehyde based thiosemicarbazones {5-R'-2-HO-C6H4-C-2(H)=N-3-(NH)-H-2-C-1(=S)-(NHR)-H-1; R = H, Me, Et, Ph: H2L1, H2L2, H2L3, H2L4 respective thio-ligands] using bipyridines/phenanthrolines (L') as co-ligands are being tested against various microorganisms (bacteria/fungi). For R' = methoxy, several complexes (five coordinate complexes) were tested recently against Gram positive bacteria such as Staphylococcus aureus (MTCC740), methicillin resistant Staphylococcus aureus (MRSA), Gram negative bacteria, Shigella flexneri (MTCC1457), Klebsiella pneumoniae (MTCC109), P. aeruginosa (MTCC741) and yeast, Candida albicans (MTCC227). These complexes displayed significant growth inhibitory action even with low MIC (minimum inhibitory concenteration). A series of new copper(II) complexes (R' = nitro, keeping R and coligands same) namely, [Cu(kappa(3)-O, N,S-L)(kappa(2)-N,N-L')] {(L)(2-) = (L-1)(2-), L' = bipy, 1, phen, 2; (L)(2-) = (L-2)(2-), L' = bipy, 3, phen, 4; (L)(2-) = (L-3)(2-), L' = bipy, 5, phen, 6; (L)(2-) = (L-4)(2-), L' = bipy, 7, phen, 8} have been isolated and characterized by elemental analysis, infrared and electronic absorption spectroscopy, ESR spectroscopy, fluorescence, and single crystal X-ray crystallography. These copper(II) complexes have been investigated for their antimicrobial activity (antibacterial and antifungal activity), viable cell count studies through time kill assays and cellular toxicity testing using MTT assays against the above mentioned bacteria/fungi. Several complexes have shown bactericidal effects with low cytotoxicity towards living cells (sheep blood used).
机译:这项研究的基本目的是探索潜在的基于金属硫代半氨基甲酸酯的金属有机抗菌剂。鉴于革兰氏阳性和革兰氏阴性细菌所表现出的抗细菌性已成为一个严重的全球性医学难题,这项研究具有重要意义。耐药菌的增加是造成各种医院感染的原因,其中,耐甲氧西林的金黄色葡萄球菌(MRSA)是最常见的医院病原体。同样,发现白色念珠菌(真菌)对多种抗真菌剂产生抗药性。在本文中,铜(II)与基于水杨醛的硫代半氨基甲酮{5-R'-2-HO-C6H4-C-2(H)= N-3-(NH)-H-2-C-1(= S)-(NHR)-H-1; [R = H,Me,Et,Ph:H 2 L 1,H 2 L 2,H 2 L 3,H 2 L 4分别是硫代-配体]使用联吡啶/菲咯啉(L')作为共配体针对各种微生物(细菌/真菌)进行测试。对于R'=甲氧基,最近针对革兰氏阳性细菌,如金黄色葡萄球菌(MTCC740),耐甲氧西林的金黄色葡萄球菌(MRSA),革兰氏阴性细菌,弗氏志贺氏菌(MTCC1457),肺炎克雷伯氏菌(MTCC109),测试了几种配合物(五种配合物) ),铜绿假单胞菌(MTCC741)和酵母白念珠菌(MTCC227)。这些复合物即使在低MIC(最小抑制浓度)下也显示出显着的生长抑制作用。一系列新的铜(II)配合物(R'=硝基,R和大肠菌素相同),即[Cu(kappa(3)-O,N,SL)(kappa(2)-N,N-L') ] {(L)(2-)=(L-1)(2-),L'= bipy,1,phen,2; (L)(2-)=(L-2)(2-),L'= bipy,3,phen,4; (L)(2-)=(L-3)(2-),L'= bipy,5,phen,6; (L)(2-)=(L-4)(2-),L'= bipy,7,phen,8}已被分离并通过元素分析,红外和电子吸收光谱,ESR光谱,荧光和单晶X射线晶体学。研究了这些铜(II)配合物的抗微生物活性(抗菌和抗真菌活性),通过时间杀灭测定法进行的活细胞计数研究以及使用MTT测定法针对上述细菌/真菌进行细胞毒性测试。几种复合物已显示出对活细胞(使用的羊血)具有低细胞毒性的杀菌作用。

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