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首页> 外文期刊>American Journal of PharmTech Research >Identification of New Pharmacophore in Bioactive Palladium Schiff Base Metal Complexes of Cephalosporins: Synthesis, Characterization and Biological Activity
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Identification of New Pharmacophore in Bioactive Palladium Schiff Base Metal Complexes of Cephalosporins: Synthesis, Characterization and Biological Activity

机译:头孢菌素的生物活性钯席夫碱金属配合物中的新药基的鉴定:合成,表征和生物活性。

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ABSTRACT Growing numbers of antibiotic-resistant bacteria are putting this golden era of medicine at risk and stresses the need for regular monitoring of antibiotic susceptibility, and developing a new design being active against resist pathogens. In this view seven Schiff base ligands of Cephalosporin group antibiotics were synthesized by their condensation with salicylaldehyde in equimolar ratio. Complexes of these Schiff bases with Pd (II) metal were synthesized in 1:2 stoichiometric ratio. The complexes were formulated as [Pd(L)2].3H2O, where L is Schiff base of seven different cephalosporin antibiotics. Complexes were characterized by elemental analyses, molar conductance, UV-Visible, FT-IR, 1H-NMR, 13C{1H}-NMR, 2D-NMR and ESI-Mass spectrometry. Schiff bases were coordinated with metal through phenolic oxygen and azomethine-N, giving simple square planar geometry to complexes. Complexes were tested for antibacterial activity and MIC against gram-negative bacteria E. coli and gram positive bacteria S. aureus and were found more potent than Schiff bases and precursor antibiotics. Keywords: Cephalosporin groups, Palladium Complexes, Schiff base, Antibacterial activity, Pharmacophore.
机译:摘要越来越多的抗生素抗性细菌使这一医学黄金时代处于危险之中,并强调需要定期监测抗生素敏感性,并开发出一种新的设计来抵抗病原体。在这种观点下,头孢菌素类抗生素的七个席夫碱配体通过与水杨醛等摩尔比缩合而合成。这些Schiff碱与Pd(II)金属的配合物以1:2的化学计量比合成。配合物配制成[Pd(L)2] .3H2O,其中L是七种不同头孢菌素抗生素的席夫碱。通过元素分析,摩尔电导,UV-可见,FT-IR,1H-NMR,13C {1H} -NMR,2D-NMR和ESI-质谱分析表征复合物。 Schiff碱通过酚氧和偶氮甲碱-N与金属配位,使配合物具有简单的正方形平面几何形状。测试了复合物对革兰氏阴性细菌大肠杆菌和革兰氏阳性细菌金黄色葡萄球菌的抗菌活性和MIC,发现它们比席夫碱和前体抗生素更有效。关键字:头孢菌素基团,钯配合物,席夫碱,抗菌活性,药效基团。

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