Kumar Dinesh, Sharma Nutan, Nair Manjula
Department of Chemistry, Banasthali University, Banasthali, 304022, India.
Department of Chemistry, American College of Dubai, 36778, Dubai, UAE.
J Biol Inorg Chem. 2017 Jun;22(4):535-543. doi: 10.1007/s00775-017-1440-9. Epub 2017 Jan 18.
Urinary tract infections commonly occur in humans due to microbial pathogens invading the urinary tract, which can bring about a range of clinical symptoms and potentially fatal sequelae. The present study is aimed at addressing the development of a new antimicrobial agent against extended spectrum beta lactamase (ESBL) producing E. coli bacteria. We have synthesised some biologically potent (NNNN) donor macrocycles (L = dibenzo[f,n]dipyrido[3,4-b:4',3'-j][1,4,9,12]tetraazacyclohexadecine-6,11,18,23(5H,12H, 7H, 24H)-tetraone, and L = 6,12,19,25-tetraoxo-4,6,11,12,16,18,23,24-octahydrotetrabenzo [b,g,k,p][1,5,10,14]tetra azacyclooctadecine-2,13-dicarboxylic acid) and their Ti and Zr metal complexes in alcoholic media using microwave protocol. Macrocyclic ligands were synthesised by incorporating of 3,5-diaminobenzoic acid, phthalic acid and 3,4-diaminopyridine in 1:1:1 molar ratio. The macrocyclic ligands and their metal complexes have been characterised by elemental analysis, conductance measurement, magnetic measurement and their structure configurations have been determined by various spectroscopic (FTIR, H/C NMR, UV-Vis, LC-MS mass, XRD and TGA) techniques. [ZrLCl]Cl metal complex shows excellent antibacterial activity against ESBLs. A zone of inhibition and minimum inhibitory concentration was determined by McFarland and the dilution method, respectively. The spectral studies confirm the binding sites of the nitrogen atom of the macrocycles. An octahedral geometry has been assigned to the metal complexes based on the findings.
由于微生物病原体侵入尿路,尿路感染在人类中普遍发生,这会引发一系列临床症状并可能导致致命的后遗症。本研究旨在研发一种针对产超广谱β-内酰胺酶(ESBL)的大肠杆菌的新型抗菌剂。我们使用微波协议在醇介质中合成了一些具有生物活性的(NNNN)供体大环化合物(配体L = 二苯并[f,n]二吡啶并[3,4-b:4',3'-j][1,4,9,12]十四氮杂十六环二烯-6,11,18,23(5H,12H,7H,24H)-四酮,以及配体L = 6,12,19,25-四氧代-4,6,11,12,16,18,23,24-八氢四苯并[b,g,k,p][1,5,10,14]十四氮杂十八环二烯-2,13-二羧酸)及其钛和锆金属配合物。通过以1:1:1的摩尔比加入3,5-二氨基苯甲酸、邻苯二甲酸和3,4-二氨基吡啶合成了大环配体。通过元素分析、电导率测量、磁测量对大环配体及其金属配合物进行了表征,并通过各种光谱技术(傅里叶变换红外光谱、氢/碳核磁共振光谱、紫外-可见光谱、液相色谱-质谱联用、X射线衍射和热重分析)确定了它们的结构构型。[ZrLCl]Cl金属配合物对ESBLs表现出优异的抗菌活性。分别通过麦克法兰法和稀释法测定了抑菌圈和最低抑菌浓度。光谱研究证实了大环化合物中氮原子的结合位点。基于这些发现,已确定金属配合物具有八面体几何构型。