Synthesis, Characterization And Antibacterial Activity Of Aspirin And Paracetamol-metal Complexes

Novel complexes of Co (11), Ni (11) and Fe (111) with aspirin and paracetamol have synthesized and characterized using infrared, electronic and Hnmr spectral, melting point and conductivity measurements. The two ligands have been found to act as bidentate chelating agents. Aspirin complexes coordinate through the carbonyl oxygen of the carboxyl and the ester groups, while paracetamol complexes coordinate through the oxygen of the hydroxyl and the amide groups. Antibacterial screening of the complexes against Bacillus substilis , serratia species and Escherichia coli , was also investigated. The metal complexes were found to have varied degree of inhibitory effect against the bacteria

Synthesis, characterization and antimicrobial activity of mixed transition metal complexes of salicylic acid with 1, 10-phenanthroline

A new series of Mn(II), Fe(II), Co(II), Cu(II) and Zn(II) mixed ligands-metal complexes derived from salicylic acid (SA) and 1,10-phenanthroline (PHEN) have been synthesized and characterized by spectroscopic studies. The coordination of the two ligands towards central metal ions has been proposed in the light of elemental analysis, IR, UV–vis spectroscopic studies. The results of the physical and spectroscopic data confirmed that the ligands are chelating agents. In 1, 10-phenanthroline, coordination occurred through the two pyridinic nitrogen groups, while in the salicylic acid coordination occurred through the oxygen of the hydroxyl and the carboxylic groups. All the complexes synthesized were of octahedral geometry. Antimicrobial activity of the mixed ligands metal complexes and the free ligands were carried out against the bacterial Escherichia coli, staphylococcus aureus, klebsiella pneumonia, pseudomonas aeruginosa and the fungi candida spp. The mixed ligands metal complexes showed higher activities when compared to the free ligands of salicylic acid but were less active than the free 1,10-phenanthroline ligand. The complexes of Cu (II) showed the highest antimicrobial activity while the Fe(II ) complex showed the least activity against the bacterial and fungi organisms.Keywords: 1,10-phenanthroline, Salicylic acid, Mixed ligands-metal complexes, Transition metal, Spectroscopy, Antimicrobia

Synthesis, Characterization And Antibacterial Activity Of Aspirin And Paracetamol-metal Complexes

Novel complexes of Co (11), Ni (11) and Fe (111) with aspirin and paracetamol have synthesized and characterized using infrared, electronic and Hnmr spectral, melting point and conductivity measurements. The two ligands have been found to act as bidentate chelating agents. Aspirin complexes coordinate through the carbonyl oxygen of the carboxyl and the ester groups, while paracetamol complexes coordinate through the oxygen of the hydroxyl and the amide groups. Antibacterial screening of the complexes against Bacillus substilis , serratia species and Escherichia coli , was also investigated. The metal complexes were found to have varied degree of inhibitory effect against the bacteria

Recent advances on therapeutic potentials of gold and silver nanobiomaterials for human viral diseases

Viral diseases are prominent among the widely spread infections threatening human well-being. Real-life clinical successes of the few available therapeutics are challenged by pathogenic resistance and suboptimal delivery to target sites. Nanotechnology has aided the design of functionalised and non-functionalised Au and Ag nanobiomaterials through physical, chemical and biological (green synthesis) methods with improved antiviral efficacy and delivery. In this review, innovative designs as well as interesting antiviral activities of the nanotechnology-inclined biomaterials of Au and Ag, reported in the last 5 years were critically overviewed against several viral diseases affecting man. These include influenza, respiratory syncytial, adenovirus, severe acute respiratory syndromes (SARS), rotavirus, norovirus, measles, chikungunya, HIV, herpes simplex virus, dengue, polio, enterovirus and rift valley fever virus. Notably identified among the nanotechnologically designed promising antiviral agents include AuNP-M2e peptide vaccine, AgNP of cinnamon bark extract and AgNP of oseltamivir for influenza, PVP coated AgNP for RSV, PVP-AgNPs for SARS-CoV-2, AuNRs of a peptide pregnancy-induced hypertension and AuNP nanocarriers of antigen for MERS-CoV and SARS-CoV respectively. Others are AgNPs of collagen and Bacillus subtilis for rotavirus, AgNPs labelled Ag30–SiO2 for murine norovirus in water, AuNPs of Allium sativum and AgNPs of ribavirin for measles, AgNPs of Citrus limetta and Andrographis Paniculata for Chikungunya, AuNPs of efavirenz and stavudine, and AgNPs-curcumin for HIV, NPAuG3-S8 for HSV, AgNPs of Moringa oleifera and Bruguiera cylindrica for dengue while AgNPs of polyethyleneimine and siRNA analogues displayed potency against enterovirus. The highlighted candidates are recommended for further translational studies towards antiviral therapeutic designs

Iron(III) and copper(II) complexes bearing 8-quinolinol with amino-acids mixed ligands: Synthesis, characterization and antibacterial investigation

AbstractFour d-orbital metal complexes with mixed ligands derived from 8-hydroxyquinoline (HQ) and amino acids (AA): l-alanine and methionine have been synthesized through a mild reflux in alkaline solution and characterized by elemental analyses, infrared, electronic transition, and temperature dependant magnetic susceptibility. The IR spectroscopy revealed that iron and copper ions coordinated through carbonyl (CO), hydroxyl group (OH) of the amino acids, N-pyridine ring of hydroxyquinoline. The elemental analysis measurement with other obtained data suggested an octahedral geometry for the iron(III) complexes and tetrahedral geometry for the copper(II) complexes. From the molar magnetic susceptibility measurement, the iron(III) system (S=5/2) d5 (non-degenerate 6A1) with χmT=0.38cm3Kmol−1 showed an antiferromagnetic while Cu2+ ions system (S=½) (2T2g) has χmT=4.77cm3Kmol−1 described as paramagnetic behaviour. In vitro antimicrobial investigations of the metal complexes against standard bacteria species gave significant inhibition with, copper complex showing highest inhibitions against Pseudomonas aeruginosa (ATCC27853) of 43mm at 10μg/ml signalling its potential as pharmaceutical or chemotherapeutic agents

Computational modelling of potential Zn-sensitive non-β-lactam inhibitors of imipenemase-1 (IMP-1)

Antibiotic resistance (AR) remains one of the leading global health challenges, mostly implicated in disease-related deaths. The Enterobacteriaceae-producing metallo-β-lactamases (MBLs) are critically involved in AR pathogenesis through Zn-dependent catalytic destruction of β-lactam antibiotics, yet with limited successful clinical inhibitors. The efficacy of relevant broad-spectrum β-lactams including imipenem and meropenem are seriously challenged by their susceptibility to the Zn-dependent carbapenemase hydrolysis, as such, searching for alternatives remains imperative. In this study, computational molecular modelling and virtual screening methods were extensively applied to identify new putative Zn-sensitive broad-spectrum inhibitors of MBLs, specifically imipenemase-1 (IMP-1) from the IBScreen database. Three ligands, STOCK3S-30154, STOCK3S-30418 and STOCK3S-30514 selectively displayed stronger binding interactions with the enzymes compared to reference inhibitors, imipenem and meropenem. For instance, the ligands showed molecular docking scores of −9.450, −8.005 and −10.159 kcal/mol, and MM-GBSA values of −40.404, −31.902 and −33.680 kcal/mol respectively against the IMP-1. Whereas, imipenem and meropenem showed docking scores of −9.038 and −10.875 kcal/mol, and MM-GBSA of −31.184 and −32.330 kcal/mol respectively against the enzyme. The ligands demonstrated good thermodynamic stability and compactness in complexes with IMP-1 throughout the 100 ns molecular dynamics (MD) trajectories. Interestingly, their binding affinities and stabilities were significantly affected in contacts with the remodelled Zn-deficient IMP-1, indicating sensitivity to the carbapenemase active Zn site, however, with non-β-lactam scaffolds, tenable to resist catalytic hydrolysis. They displayed ideal drug-like ADMET properties, thus, representing putative Zn-sensitive non-β-lactam inhibitors of IMP-1 amenable for further experimental studies. Communicated by Ramaswamy H. Sarma</p