Antibacterial activity and pharmacological effect of some mixed-ligand tris-chelates of copper(II) containing neutral N,N-donors and kinetics study of the novel synthetic route for the complexes

P. Majumdar; B. Banerjee; D. Ghosh

doi:10.4314/bcse.v33i3.8

In VitroandIn VivoActivities of the Novel Ketolide RBx 14255 against Clostridium difficile

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00015-12 ◽

2012 ◽

Vol 56 (11) ◽

pp. 5986-5989 ◽

Cited By ~ 5

Author(s):

Manoj Kumar ◽

Tarun Mathur ◽

Tarani K. Barman ◽

G. Ramkumar ◽

Ashish Bhati ◽

...

Keyword(s):

Clostridium Difficile ◽

Time Dependent ◽

Kinetics Study ◽

The Novel ◽

Promising Candidate ◽

Hamster Model ◽

Bacterial Killing ◽

Content Type ◽

Time Kill

ABSTRACTThe MIC90of RBx 14255, a novel ketolide, againstClostridium difficilewas 4 μg/ml (MIC range, 0.125 to 8 μg/ml), and this drug was found to be more potent than comparator drugs. Anin vitrotime-kill kinetics study of RBx 14255 showed time-dependent bacterial killing forC. difficile. Furthermore, in the hamster model ofC. difficileinfection, RBx 14255 demonstrated greater efficacy than metronidazole and vancomycin, making it a promising candidate forC. difficiletreatment.

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Novel Low Spin Mixed Ligand Thiohydrazide Complexes of Iron(III): Synthesis, Spectral Characterization, Molecular Modeling, and Antibacterial Activity

International Journal of Inorganic Chemistry ◽

10.1155/2014/580232 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 1

Author(s):

Dolan Sengupta ◽

Snigdha Gangopadhyay ◽

Sanchita Goswami ◽

Arnab Dutta ◽

Vikash Kumar ◽

...

Keyword(s):

Antibacterial Activity ◽

Magnetic Susceptibility ◽

Molecular Modeling ◽

Antibacterial Properties ◽

Mixed Ligand ◽

Magnetic Susceptibility Data ◽

Susceptibility Data ◽

Octahedral Environment ◽

Biological Studies ◽

Iron Center

Mixed ligand complexes of Fe(III) with aromatic thiohydrazides of general composition [Fe(acac)(L)2] have been synthesized and characterized (acac-acetylacetonate, L = bidentate uninegative aromatic thiohydrazide ligand, for example, thiobenzhydrazide, 2-hydroxythiobenzhydrazide, furan-2-thiohydrazide, and thiophen-2-thiohydrazide). The magnetic susceptibility data and the EPR spectra of these complexes suggested the formation of rhombically distorted low spin iron center (d5) in octahedral environment, which was also supported by the UV-vis spectral data of the complexes. Biological studies of these complexes also indicated that the iron-thiohydrazido complexes have superior antibacterial properties compared to the corresponding ligands.

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Synthesis, Characterization and Antibacterial Activity of Mixed Ligand Complexes of Pd(II) Ions with Oxalic Acid and Heterocyclic Amines

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v17i1.22314 ◽

2015 ◽

Vol 17 (1) ◽

pp. 46-50

Author(s):

Md Belayet Hossain ◽

Md Abdus Salam ◽

Farzana Siddiquee ◽

MA Yousuf

Keyword(s):

Antibacterial Activity ◽

Oxalic Acid ◽

Metal Ion ◽

Pathogenic Bacteria ◽

Magnetic Measurements ◽

Spectroscopic Studies ◽

Mixed Ligand ◽

Heterocyclic Amines ◽

Mixed Ligand Complexes ◽

Diffusion Method

The present work has been designed for the characterization and antibacterial studies of mixed ligand complexes of Pd(II) ions with phthalic acid and heterocyclic amines. The general formula of the complexes is (MLL/) [where, M = Pd(II); L = Oxalic acid, C2O4, L/ = Quinoline, C9H7N(1); iso-Quinoline, C9H7N(2)]. The complexes were prepared in the solid form and characterized by elemental analysis, conductivity & magnetic measurements and infrared & electronic spectroscopic studies. The infrared spectra of the complexes confirmed the coordination of metal ion with ligands. Their antibacterial activity has been evaluated by the disc diffusion method against seven pathogenic bacteria (three gram positive and four gram negative). The complexes were shown to exhibit mild to moderate antibacterial activity against the tested bacteria. DOI: http://dx.doi.org/10.3329/bpj.v17i1.22314 Bangladesh Pharmaceutical Journal 17(1): 46-50, 2014

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High-spin binuclear Co(II) complexes with a pendant octaazamaclocycle and carboxylates

Journal of the Serbian Chemical Society ◽

10.2298/jsc0712295v ◽

2007 ◽

Vol 72 (12) ◽

pp. 1295-1308 ◽

Cited By ~ 5

Author(s):

G. Vuckovic ◽

S.B. Tanaskovic ◽

Z.M. Miodragovic ◽

V. Stanic

Keyword(s):

Antibacterial Activity ◽

Terephthalic Acid ◽

Chair Conformation ◽

Molar Conductivity ◽

Mixed Ligand ◽

Boat Conformation ◽

Trans Position ◽

Oxidation Of Co ◽

Elemental Analyses ◽

Cv Measurements

Three new binuclear Co(II) mixed-ligand complexes with N,N?,N??,N???-tetrakis( 2-pyridylmethyl)-1,4,8,11-tetraazacyclotetradecane (tpmc) and mono- or dicarboxylate ligands were prepared and some of their physical properties were determined. The general formulas: [Co2(HCOO)2tpmc](ClO4)2?4H2O, [Co2(CH3COO)2tpmc](ClO4)2 and [Co2(tpht)tpmc](ClO4)2?4H2O (tphtH2 = terephthalic acid) were proposed on the basis of elemental analyses (C,H,N) and molar conductivity. UV/Vis absorption and IR spectra, magnetic and CV measurements were used to study their geometries and properties. For the monocarboxylate complexes, an exo coordination of Co(II) with four nitrogens from tpmc and bis-bidentate bonded HCOO-/CH3COO- in the trans position is assumed. Tpmc adopts the chair conformation. For the dicarboxylate complex, it is supposed that a terephthalate dianion, as well as methylene chains from cyclam bridge two Co(II) atoms, while tpmc is in the boat conformation. The complexes were stable against chemical and electrochemical oxidation of Co(II) to Co(III). The data are compared with those for the previously published Cu(II) complexes containing the corresponding ligands and mutual similarities or differences were considered. Finally, some antibacterial activity of the complexes was found.

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In VitroAntibacterial Activity of the Ceftazidime-Avibactam Combination against Enterobacteriaceae, Including Strains with Well-Characterized β-Lactamases

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.04218-14 ◽

2015 ◽

Vol 59 (4) ◽

pp. 1931-1934 ◽

Cited By ~ 39

Author(s):

Premavathy Levasseur ◽

Anne-Marie Girard ◽

Christine Miossec ◽

John Pace ◽

Ken Coleman

Keyword(s):

Antibacterial Activity ◽

Antimicrobial Agents ◽

The Novel ◽

Content Type ◽

Class A ◽

Fixed Weight ◽

Class D ◽

Resistant Strains ◽

Esbl Producers

ABSTRACTThe novel β-lactamase inhibitor avibactam is a potent inhibitor of class A, class C, and some class D enzymes. Thein vitroantibacterial activity of the ceftazidime-avibactam combination was determined for a collection ofEnterobacteriaceaeclinical isolates; this collection was enriched for resistant strains, including strains with characterized serine β-lactamases. The inhibitor was added either at fixed weight ratios to ceftazidime or at fixed concentrations, with the latter type of combination consistently resulting in greater potentiation of antibacterial activity. In the presence of 4 μg/ml of avibactam, the ceftazidime MIC50and MIC90(0.25 and 2 μg/ml, respectively) were both below the CLSI breakpoint for ceftazidime. Further comparisons with reference antimicrobial agents were performed using this fixed inhibitor concentration. Against most ceftazidime-susceptible and -nonsusceptible isolates, the addition of avibactam resulted in a significant increase in ceftazidime activity, with MICs generally reduced 256-fold for extended-spectrum β-lactamase (ESBL) producers, 8- to 32-fold for CTX-M producers, and >128-fold for KPC producers. Overall, MICs of a ceftazidime-avibactam combination were significantly lower than those of the comparators piperacillin-tazobactam, cefotaxime, ceftriaxone, and cefepime and similar or superior to those of imipenem.

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Synthesis, identification and application of the novel metal-organic framework Fe3O4@PAA@ZIF-8 for the drug delivery of ciprofloxacin and investigation of antibacterial activity

Artificial Cells Nanomedicine and Biotechnology ◽

10.1080/21691401.2019.1617729 ◽

2019 ◽

Vol 47 (1) ◽

pp. 2024-2030 ◽

Cited By ~ 9

Author(s):

Maryam Esfahanian ◽

Mohammad Ali Ghasemzadeh ◽

Seyyed Mohammad Hossein Razavian

Keyword(s):

Drug Delivery ◽

Antibacterial Activity ◽

Metal Organic Framework ◽

The Novel ◽

Metal Organic ◽

Organic Framework

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New Chloramphenicol Derivatives from the Viewpoint of Anticancer and Antimicrobial Activity

Antibiotics ◽

10.3390/antibiotics8010009 ◽

2019 ◽

Vol 8 (1) ◽

pp. 9

Author(s):

Panagiota Giannopoulou ◽

Dionissia Missiri ◽

Georgia Kournoutou ◽

Eleni Sazakli ◽

Georgios Papadopoulos ◽

...

Keyword(s):

Antimicrobial Activity ◽

Antibacterial Activity ◽

Adverse Effects ◽

Anticancer Activity ◽

Bacterial Growth ◽

Anticancer Agent ◽

The Novel ◽

Anticancer Properties ◽

Antibacterial And Anticancer Activity ◽

Alkyl Length

Over the last years, we have been focused on chloramphenicol conjugates that combine in their structure chloramphenicol base with natural polyamines, spermine, spermidine and putrescine, and their modifications. Conjugate 3, with spermidine (SPD) as a natural polyamine linked to chloramphenicol base, showed the best antibacterial and anticancer properties. Using 3 as a prototype, we here explored the influence of the antibacterial and anticancer activity of additional benzyl groups on N1 amino moiety together with modifications of the alkyl length of the aminobutyl fragment of SPD. Our data demonstrate that the novel modifications did not further improve the antibacterial activity of the prototype. However, one of the novel conjugates (4) showed anticancer activity without affecting bacterial growth, thus emerging as a promising anticancer agent, with no adverse effects on bacterial microflora when taken orally.

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Synthesis of Mixed Ligand Ruthenium (II/III) Complexes and Their Antibacterial Evaluation on Drug-Resistant Bacterial Organisms

Journal of Chemistry ◽

10.1155/2020/2150419 ◽

2020 ◽

Vol 2020 ◽

pp. 1-10 ◽

Cited By ~ 1

Author(s):

James T. P. Matshwele ◽

Florence Nareetsile ◽

Daphne Mapolelo ◽

Pearl Matshameko ◽

Melvin Leteane ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Magnetic Susceptibility ◽

Klebsiella Pneumoniae ◽

Bacterial Species ◽

Mixed Ligand ◽

Resistant Bacteria ◽

Drug Resistant ◽

Bacterial Dna ◽

Polypyridyl Ligand

The potential antimicrobial properties of a tridentate polypyridyl ligand 4-butoxy-N,N-bis(pyridin-2-ylmethyl)aniline (BUT) 1 and its corresponding mixed ligand ruthenium complexes were investigated on drug-resistant and non-drug-resistant bacterial species. The ligand and its complexes were synthesized and successfully characterized by 1H NMR, UV/Vis, and FTIR spectra; ESI-MS; and magnetic susceptibility. Electronic spectra and magnetic susceptibility of these Ru(II)/(III) complexes suggest that they are of a low spin crystal field split, where the Ru(III) is a d5 and Ru(II) d6 low spin. These compounds were tested for antibacterial activity on two bacterial species: Staphylococcus aureus (S. aureus) and Klebsiella pneumoniae (K. pneumoniae), as well as their drug-resistant strains methicillin-resistant Staphylococcus aureus (MRSA) and multidrug resistant Klebsiella pneumoniae (MDR K. pneumoniae). All the compounds inhibited growth of the two non-drug-resistant bacteria and only one drug-resistant strain MRSA. However, only the ligands BUT and 2,2-dipyridylamine showed activity against MRSA, while all complexes did not show any antibacterial activity on MRSA. We observed large zones of inhibition for the Gram-positive S. aureus and MRSA bacteria, compared to the Gram-negative K. pneumoniae bacteria. DNA cleavage studies with gel electrophoresis showed denatured bacterial DNA on the gel from all the complexes, with the exception of the ligand, suggesting DNA nuclease activity of the complexes in the bacterial DNA.

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A Facile and Efficient Synthesis of bis(Imidazo[1,2-a]pyridin-3-yl)methane and vinyl derivatives

Letters in Organic Chemistry ◽

10.2174/1570178618666211022144225 ◽

2021 ◽

Vol 18 ◽

Author(s):

D.E. Prasada Rao ◽

M. David Raju ◽

J. Surendra ◽

A. Vasu Babu ◽

P. Eswaraiah ◽

...

Keyword(s):

Acetic Acid ◽

Trifluoroacetic Acid ◽

Methyl Chloride ◽

The Novel ◽

Synthetic Route ◽

Efficient Synthesis ◽

Vinyl Derivatives

An efficient synthetic route for the novel bis-imdizo[1,2-a]pyridine-3-yl)methane (2a-k) derivatives have been developed using acetic acid and two drops of trifluoroacetic acid at 40-45oC, resulting in 60-72% yields. An attempt to synthesize bis(Imidazo[1,2-a]pyridin-3-yl)methyl chloride derivatives by the reaction between two moles of imidazo[1,2-a]pyridine, one mole of chloroacetaldehyde in acetic acid, and two drops of trifluoroacetic acid was not successful, instead underwent dehydrohalogenation to yield vinyl derivatives (4a-d).

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