scholarly journals Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

2021 ◽  
Vol 22 (18) ◽  
pp. 9709
Author(s):  
Dariusz Karcz ◽  
Karolina Starzak ◽  
Ewa Ciszkowicz ◽  
Katarzyna Lecka-Szlachta ◽  
Daniel Kamiński ◽  
...  
Keyword(s):  
Staphylococcus Epidermidis ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Acetylcholinesterase Inhibitors ◽  
Spectroscopic Techniques ◽  
Central Metal ◽  
Inhibition Activity ◽  
Ache Inhibition ◽  
Bacterial Strains ◽  
Gram Negative

A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity

scholarly journals Synthesis, structural determination and antibacterial activity of compounds derived from vanillin and 4-aminoantipyrine

2004 ◽  
Vol 69 (12) ◽  
pp. 991-998 ◽  
Author(s):  
Yogesh Vaghasiya ◽  
Rathish Nair ◽  
Mayur Soni ◽  
Shipra Baluja ◽  
Sumitra Shanda
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Side Chain ◽  
Structural Determination ◽  
Bacterial Strains ◽  
Polar Solvents ◽  
Gram Negative

Schiff bases derived from 4-aminoantipyrine and vanillin were evaluated for their potential as antibacterial agents against some Gram positive and Gram negative bacterial strains. The antibacterial activity was studied against P. pseudoalcaligenes ATCC 17440, P. vulgaris NCTC 8313, C. freundii ATCC 10787 E. aerogenes ATCC 13048, S. subfava NCIM 2178 and B. megaterium ATCC 9885. The determination of the antibacterial activity was done using the Agar Ditsh method. The Schiff bases produced were: (1) 4-(4-hydroxy 3-methoxybenzylideneamino) -1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one [VV1]; (2) 4-(benzylideneamino) -1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one [VY2]); (3) 4-[(furan-3-ylmethylene) amino ]-1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one [VY3]?; (4) 4-(4-methoxybenzylideneamino) -1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one [VY4]?; (5) 2-methoxy-4-[(4-methoxyphenylimino) methyl ]phenol [VY5]; (6) 4-[(2,4-dimethylphenylimino) methyl]-2-methoxyphenol [VY6]); (7) 2-methoxy-4-(naphthalene-1-yliminomethyl) phenol [VY7]?and (8) 4-[(4-hydroxy-3-methoxybenzylidene)amino]-N-(5-methylisoxazol 3-yl)benzenesulfonamide [VY8]. The antibacterial activity was evaluated in two polar solvents, DMSO and DMF. The Schiff bases derived from vanillin as the central molecule with 2,4-dimethylaniline and sulphamethoxazole as the side chain in DMSO effectively inhibited the investigated bacteria and appear to be promising antimicrobial agents.

scholarly journals Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

2018 ◽  
Vol 86 (4) ◽  
pp. 42
Author(s):  
Oludotun Phillips ◽  
Edet Udo ◽  
Roselyn D’silva
Keyword(s):  
Antibacterial Activity ◽  
Staphylococcus Epidermidis ◽  
Moraxella Catarrhalis ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antibacterial Resistance ◽  
Bacterial Strains ◽  
Resistance Development ◽  
Antibacterial Drugs ◽  
Gram Negative

Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs’ approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of d-/l-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d (d- and l-alaninyl derivatives bearing the 3,5-dinitrobenzoyl substituent), 10e (l-alaninyl derivative bearing the 5-nitrofurancarbonyl group) and 9f and 10f (d- and l-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC: 2 µg/mL) against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and Moraxella catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the d- and l-alaninyl derivatives as a result of the stereochemistry of the compounds.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

Synthesis, in silico pharmacokinetics and biological evaluation of some new thiazolidinedione as PPAR-γ agonists and antibacterial agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
New Drugs ◽  
Diabetic Patients ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Ppar Γ

Background: The frequent uses of antimicrobial agents to treat infections in diabetic patients make them more drug resistance than non diabetic patients which accounts for higher mortality rate of diabetic patients. Therefore, it is a necessity today to synthesize new drugs with dual mode of action as antidiabetic and antibacterial agents. In the present work, new derivatives containing thiazolidinedione and 1,3,4-oxadiaozle have been synthesized and screened for PPAR-γ and antibacterial activities. Methods: Compound 5-12 have been synthesized from 2-methoxy benzaldehyde and thiazolidinedione and characterized using different spectroscopic techniques such as IR, NMR and mass spectrometry. These compounds were tested for in vitro PPAR-γ transactivation, PPAR-γ gene expression and antibacterial activities. Finally molecular docking was carried out to see the binding interactions of molecules with the target protein. Results: All the compounds follow Lipinski rule suggesting the synthesized derivatives have good drug likeness properties. Compound 11 and 12 exhibited promising PPAR-γ transactivation with 73.69% and 76.50%, respectively as well as showed significant antibacterial activity with comparable MIC of 3.12 μg/disc to standard drug amoxicillin. The docking result was found to be in consistent with the in vitro PPAR-γ transactivation results. Conclusion: Compounds 11 and 12 can be further investigated as lead molecules for the development of new and effective antidiabetic and antibacterial agents.

scholarly journals Purification of Bioactive Peptide with Antimicrobial Properties Produced by Saccharomyces cerevisiae

Foods ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 324 ◽  
Author(s):  
Shayma Thyab Gddoa Al-sahlany ◽  
Ammar Altemimi ◽  
Alaa Al-Manhel ◽  
Alaa Niamah ◽  
Naoufal Lakhssassi ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Antimicrobial Properties ◽  
Antibacterial Peptide ◽  
Inhibition Activity ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Viable Cells ◽  
Ph Range

A variety of organisms produce bioactive peptides that express inhibition activity against other organisms. Saccharomyces cerevisiae is considered the best example of a unicellular organism that is useful for studying peptide production. In this study, an antibacterial peptide was produced and isolated from Saccharomyces cerevisiae (Baker’s yeast) by an ultrafiltration process (two membranes with cut-offs of 2 and 10 kDa) and purified using the ÄKTA Pure 25 system. Antibacterial peptide activity was characterized and examined against four bacterial strains including Gram-positive and Gram-negative bacteria. The optimum condition for yeast growth and antibacterial peptide production against both Escherichia. coli and Klebsiella aerogenes was 25–30 °C within a 48 h period. The isolated peptide had a molecular weight of 9770 Da, was thermostable at 50–90 °C for 30 min, and tolerated a pH range of 5–7 at 4 °C and 25 °C during the first 24 h, making this isolated antibacterial peptides suitable for use in sterilization and thermal processes, which are very important aspect in food production. The isolated antibacterial peptide caused a rapid and steady decline in the number of viable cells from 2 to 2.3 log units of gram-negative strains and from 1.5 to 1.8 log units of gram-positive strains during 24 h of incubation. The isolated antibacterial peptide from Saccharomyces cerevisiae may present a potential biopreservative compound in the food industry exhibiting inhibition activity against gram-negative and gram-positive bacteria.

Activity of free fatty acids-rich non-polar fractions from fruits of Capsicum chinense var. Criolla and Jaguar

2019 ◽  
Vol 66 (3-4) ◽  
pp. 220-226
Author(s):  
J. Efrain Ramirez-Benitez ◽  
Ibis Vargas Paredes ◽  
Luis F. Cuevas Glory ◽  
Enrique Sauri Duch ◽  
Victor M. Moo Huchin ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Staphylococcus Epidermidis ◽  
Bioactive Molecules ◽  
Biological Functions ◽  
Capsicum Chinense ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Plant Essential Oils ◽  
Unripe Fruits

Plant-essential oils have been considered as an important source of bioactive molecules like antimicrobials, analgesics, anti-inflammatory and anti-carcinogen agents. Biological functions of plant extracts from the genus Capsicum are unknown. In the present work, non-polar fractions of ripe and unripe fruits of Capsicum chinense Jacq. Cultivar (cv.) Jaguar and Criollo were obtained by hexane-batch extraction and tested for antimicrobial activity against Gram-negative bacterial strain Escherichia coli (ATCC 25922), Gram-positive bacterial strains Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus epidermidis (ATCC 12228), and yeast Candida albicans (ATCC 90028). Non-polar fractions from ripe fruits for both cv. exhibited greater antimicrobial activity compared to unripe fruits. Implication of numbered FFA’s on observed antimicrobial activity are discussed.

The Activity of Alkanna Species in vitro Culture and Intact Plant Extracts Against Antibiotic Resistant Bacteria

2019 ◽  
Vol 25 (16) ◽  
pp. 1861-1865 ◽  
Author(s):  
Naira Sahakyan ◽  
Margarit Petrosyan ◽  
Armen Trchounian
Keyword(s):  
Antibiotic Resistance ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antimicrobial Agents ◽  
Resistant Bacteria ◽  
Plant Origin ◽  
Bacterial Strains ◽  
Biotechnological Production ◽  
Antibiotic Resistant

Overcoming the antibiotic resistance is nowadays a challenge. There is still no clear strategy to combat this problem. Therefore, the urgent need to find new sources of antibacterial agents exists. According to some literature, substances of plant origin are able to overcome bacterial resistance against antibiotics. Alkanna species plants are among the valuable producers of these metabolites. But there is a problem of obtaining the standardized product. So, this review is focused on the discussion of the possibilities of biotechnological production of antimicrobial agents from Alkanna genus species against some microorganisms including antibiotic resistant bacterial strains.

scholarly journals Aryl Rhodanines Specifically Inhibit Staphylococcal and Enterococcal Biofilm Formation

2009 ◽  
Vol 53 (10) ◽  
pp. 4357-4367 ◽  
Author(s):  
Timothy J. Opperman ◽  
Steven M. Kwasny ◽  
John D. Williams ◽  
Atiyya R. Khan ◽  
Norton P. Peet ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Small Molecules ◽  
Staphylococcus Epidermidis ◽  
Biofilm Formation ◽  
Antibiofilm Activity ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Artificial Surfaces ◽  
Causative Agents ◽  
Biofilm Development

ABSTRACT Staphylococcus epidermidis and Staphylococcus aureus are the leading causative agents of indwelling medical device infections because of their ability to form biofilms on artificial surfaces. Here we describe the antibiofilm activity of a class of small molecules, the aryl rhodanines, which specifically inhibit biofilm formation of S. aureus, S. epidermidis, Enterococcus faecalis, E. faecium, and E. gallinarum but not the gram-negative species Pseudomonas aeruginosa or Escherichia coli. The aryl rhodanines do not exhibit antibacterial activity against any of the bacterial strains tested and are not cytotoxic against HeLa cells. Preliminary mechanism-of-action studies revealed that the aryl rhodanines specifically inhibit the early stages of biofilm development by preventing attachment of the bacteria to surfaces.

Occurrence of Resistance to Antibiotics and Metals and of Plasmids in Bacterial Strains Isolated from Marine Environments

1993 ◽  
Vol 27 (3-4) ◽  
pp. 475-478 ◽  
Author(s):  
M. Avilés ◽  
J. C. Codina ◽  
A. Pérez-García ◽  
F. Cazorla ◽  
P. Romero ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Agents ◽  
Marine Environments ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Resistance Profile ◽  
Resistance To Antibiotics ◽  
Resistance Patterns ◽  
Arsenic Copper

Tlie resistance patterns to different antibiotics and lieavy metals of bacterial strains isolated firom marine environments (seawater, sediments and shellfishes) were studied. Pseudomonas aeruginosa showed the widest resistance profile, both to antibiotics and metals. In general, the resistance profiles of Gram-negative I microorganisms include the resistance to arsenic, copper, amoxycillin and tetracydine. Some associations of resistance to different antimicrobial agents were frequently observed. An important proportion of the studied strains harboured plasmids; and the association between the occurrence of plasmids and the resistance to arsenic, amoxycillin, carbencillin and streptomycin was observed.

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