scholarly journals 1,2,4-Triazoles as Important Antibacterial Agents

2021 ◽  
Vol 14 (3) ◽  
pp. 224
Author(s):  
Małgorzata Strzelecka ◽  
Piotr Świątek
Keyword(s):  
Drug Resistance ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Rational Design ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
The Novel ◽  
Global Spread ◽  
Antibacterial Potential

The global spread of drug resistance in bacteria requires new potent and safe antimicrobial agents. Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity. A large volume of research on triazole and their derivatives has been carried out, proving significant antibacterial activity of this heterocyclic core. This review is useful for further investigations on this scaffold to harness its optimum antibacterial potential. Moreover, rational design and development of the novel antibacterial agents incorporating 1,2,4-triazole can help in dealing with the escalating problems of microbial resistance.

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

2015 ◽  
Vol 59 (4) ◽  
pp. 1931-1934 ◽  
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.

scholarly journals Silver-calcium-borates as better replacement for conventional organic antimicrobials in cosmetic products

2022 ◽  
Vol 11 (1) ◽  
pp. 113-120 ◽  
Author(s):  
A.L. Arunachalam ◽  
S. Induja ◽  
V. Parthasarathy ◽  
P.S. Raghavan
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Xrd Analysis ◽  
New Drugs ◽  
The Novel ◽  
Cosmetic Products ◽  
Bacterial Reduction ◽  
Phase Purity ◽  
Powder Xrd Analysis ◽  
Antibacterial And Antifungal

Microbes generally develop resistance towards organic antibacterial agents like ampicillin, Sulfonamides, methicillin, etc., and progressively new drugs are being invented to replace them. Hence, replacement of organic antibacterial agents with inorganic analogues requires constant research and the present investigation reports alternatives for conventional antimicrobial agents like methylparaben, diazolidinyl urea, etc., in the cosmetic products with silver incorporated calcium borates. The chemically synthesized silver-calcium borates have been analyzed for phase purity using powder XRD analysis, nature of bonding using FTIR vibrations, and morphology using SEM. The antibacterial and antifungal studies were carried out for the novel inorganic silver-calcium borates incorporated cosmetic products. The products were also subjected to thermal & photostability studies and found to be comparable with that of commercially available products. A minimum quantity of 3 ppm of silver-calcium borate concentration was required to bring about nearly 100% bacterial reduction in the cosmetic products.

Novel Strategiesto Combat the Emerging Drug Resistance in Human Pathogenic Microbes

2020 ◽  
Vol 21 ◽  
Author(s):  
Hafsa Qadri ◽  
Abdul Haseeb ◽  
Manzoor Mir
Keyword(s):  
Drug Resistance ◽  
Combination Therapy ◽  
Antimicrobial Agents ◽  
Resistance Mechanisms ◽  
Antimicrobial Drug ◽  
The Novel ◽  
Host Defenses ◽  
Bacteriophage Therapy ◽  
Antimicrobial Drug Resistance ◽  
Pathogenic Microbes

: The major health-care burden for the developing world are the Infectious diseases and antimicrobial agents prove to be the magical drugs to combat this. But the phenomenon of antimicrobial resistance (AMR) represents a global challenging issue, which requires to be addressed effectively. The antimicrobial treatment for the emerging multidrug-resistant bacterial (e.g. TB, Cholera) and fungal (e.g. Candidiasis) infections is very limited and there are multiple causes and reasons responsible for the evolution of such resistance. Considering the critical issues of increasing AMR, there is an urgent requirement of identification, development, validation, and progression of novel strategies and approaches that can easily be utilized for overcoming this serious issue. Immunotherapy represents a significant way to improve host defenses and combat the issue of antimicrobial drug resistance. Similarly, drug combination therapy represents another promising approach for reducing the evolution of resistance and enhancing the longevity of the antimicrobial agents. Bacteriophage therapy also acts as a novel therapeutic option to control the development of the multidrug resistance (MDR) phenomenon. Besides, CRISPR, an innovative genome editing technology offers multiple applications to safeguard host defenses to overcome different resistance challenges. The novel approaches/strategies like combination therapy, bacteriophage therapy, immunotherapy, and CRISPR/Cas discussed here presents an overview of some of the novel strategies/approaches to be adopted against the pathogenic microbes/microbial invasions along with advanced knowledge of different drug resistance mechanisms adopted by the microbial pathogens to gain resistance against different antimicrobial agents. Therefore, understanding the novel control plans/approaches and different drug resistance mechanisms will help achieve the goals of the successful development of potential antimicrobial drugs and their respective targets and eventually help curtail the problem of increasing antimicrobial drug resistance menace in various human pathogenic microbes.

Antioxidant and Antibacterial Activity of Sulfonamides Derived from Carvacrol: A Structure-Activity Relationship Study

2020 ◽  
Vol 20 (3) ◽  
pp. 173-181 ◽  
Author(s):  
Aldo S. de Oliveira ◽  
Luiz F. S. de Souza ◽  
Ricardo J. Nunes ◽  
Susana Johann ◽  
David L. Palomino-Salcedo ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Small Molecule ◽  
Bacterial Resistance ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Structure Activity ◽  
Relationship Study ◽  
Antibacterial Potential

Background: Bacterial resistance to antibiotics is a growing problem in all countries and has been discussed worldwide. In this sense, the development of new drugs with antibiotic properties is highly desirable in the context of medicinal chemistry. Methodology: In this paper we investigate the antioxidant and antibacterial potential of sulfonamides derived from carvacrol, a small molecule with drug-like properties. Most sulfonamides had antioxidant and antibacterial potential, especially compound S-6, derived from beta-naphthylamine. Result: To understand the possible mechanisms of action involved in biological activity, the experimental results were compared with molecular docking data. Conclusion: This research allows appropriate discussion on the identified structure activity relationships.

scholarly journals Potential Antimicrobial and Chemical Composition of Essential Oils from Piper caldense Tissues

2017 ◽  
Vol 60 (3) ◽  
Author(s):  
Dayane Silva Rocha ◽  
Janete Magali Da Silva ◽  
Daniela Maria Do Amaral Ferraz Navarro ◽  
Claúdio Augusto Gomes Camara ◽  
Camila Soledade De Lira ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Chemical Composition ◽  
Essential Oils ◽  
Chemical Constituents ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Major Chemical ◽  
Antibacterial Potential

The essential oils from leaves, stems and roots of Piper caldense were analyzed by GC-MS. The antibacterial potential of the oils was evaluated against gram-negative bacteria and gram-positive bacteria. The major chemical constituents that were identified from various parts of this plant were α-cardinal, α-muurolol, tujopsan-2-β-ol and δ-cadiene in the leaves, valencene, pentadecane, elina-3,7-11-dieno α-terpineol in the roots and terpine-4-ol, α-terpineol, α-cadinol 2-β-ol in the stems. Tissue oils showed antibacterial activity against the bacteria tested except for Enterococcus faecalis. This is the first report of the biological activity and chemical composition essential oil of P. caldense.

scholarly journals Synthesis and Biological Activity of 1,2,4-Triazolo-[3,4-b]Thiadiazole as Antimicrobial Agents

2014 ◽  
Vol 26 ◽  
pp. 45-52
Author(s):  
Piyush B. Vekariya ◽  
Jalpa R. Pandya ◽  
Vaishali Goswami ◽  
Hitendra S. Joshi
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Spectral Analysis ◽  
Biological Activity ◽  
Antimicrobial Agents ◽  
Dilution Method ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
Broth Dilution

Some novel 6-fluoro chroman derivatives having 1,2,4-triazolo-[3,4-b]thiadiazole were synthesized and characterized by IR, NMR and mass spectral analysis. All synthesized compounds were screened for antimicrobial activity using broth dilution method. All the compounds showed good antimicrobial activity and compound 5e showed significant antibacterial activity.

scholarly journals Comparative Evaluation of Antibacterial Effects of Nanoparticle-Incorporated Orthodontic Primer: An In Vitro Study

2021 ◽  
pp. 030157422098818
Author(s):  
Cheepurupalli Meher Vineesha ◽  
D Praveen Kumar Varma ◽  
P Arun Bhupathi ◽  
CV Padma Priya ◽  
M Anoosha ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Antibacterial Effects ◽  
Disk Diffusion Method

Aim and Objectives: To compare and evaluate the antibacterial efficacy of various nanoparticles incorporated in orthodontic primer with that of conventional antimicrobial agents at different concentrations on Streptococcus mutans ( S. mutans) strain. Materials and Methods: Transbond XT Primer was mixed with 2.5% and 5% benzalkonium chloride (BAC), 0.2% and 2.5% chlorhexidine, 1% and 3% titanium dioxide (TiO2) nanoparticles, 0.2% and 0.5% nanohydroxyapatite, and 0.2% and 0.5% silica-doped nanohydroxyapatite powders. Antibacterial activity against S. mutans for all the materials was evaluated by the disk diffusion method for periods of 48 (T1) and 72 (T2) hours. Results: There was a significant increase in the antimicrobial activity of the orthodontic primer modified by the addition of antibacterial agents. The highest zone of inhibition against S. mutans was observed for silica-doped nanohydroxyapatite of 0.5% (11.03 mm) among all the nanoparticles, which was similar to the conventional antibacterial agents used in our study. Conclusions: • Among all the groups, BAC at 5% concentration showed the highest antimicrobial activity, and the least activity was exhibited by 1% TiO2 nanoparticles. • Silica-doped nanohydroxyapatite at 0.5% expressed the greatest antibacterial activity among all the nanoparticles. • All the materials showed sustained antibacterial activity even after 72 hours.

scholarly journals Enhancing the antibacterial activity of antimicrobial peptide PMAP-37(F34-R) by cholesterol modification

2020 ◽  
Vol 16 (1) ◽  
Author(s):  
Liangliang Chen ◽  
Tengfei Shen ◽  
Yongqing Liu ◽  
Jiangfei Zhou ◽  
Shuaibing Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Peptide ◽  
Therapeutic Effect ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Therapeutic Effects ◽  
Microbial Infection ◽  
Cholesterol Modification

Abstract Background The problem of increasing resistance against conventional antibiotics has drawn people’s attention. Therefore, the development of novel antibacterial agents with effective and safe therapeutic effects is imminent. Antimicrobial peptides (AMPs) are considered a promising class of antibacterial agents due to their broad antibacterial spectrum. Results In this study, on the basis of our previously studied peptide PMAP-37(F34-R), a novel antimicrobial peptide Chol-37(F34-R) was developed by N-terminal cholesterol modification to increase hydrophobicity. We observed that the N-terminal cholesterol-modified Chol-37(F34-R) showed higher antimicrobial activity than PMAP-37(F34-R) in vitro. Chol-37(F34-R) also exhibited effective anti-biofilm activity and may kill bacteria by improving the permeability of their membranes. Chol-37(F34-R) exerted high stability in different pH, salt, serum, and boiling water environments. Chol-37(F34-R) also showed no hemolytic activity and substantially low toxicity. Furthermore, Chol-37(F34-R) exhibited good potency of bacteria eradication and promoted wound healing and abscess reduction in infected mice. Meanwhile, in S. aureus ATCC25923-infected peritonitis model, Chol-37(F34-R) exhibited an impressive therapeutic effect by reducing the decrease in systemic bacterial burden and alleviating organ damage. Conclusions Our findings suggested that the N-terminal cholesterol modification of PMAP-37(F34-R) could improve antibacterial activity. Chol-37(F34-R) displayed excellent bactericidal efficacy and impressive therapeutic effect in vivo. Thus, Chol-37(F34-R) may be a candidate for antimicrobial agents against microbial infection in the clinic.

scholarly journals Antibacterial Activity of Semi Purified Extract of Marine-Derived Trichoderma reesei PDSP 5.7 Using Bioguided Fractionation Method

2020 ◽  
Vol 9 (1) ◽  
pp. 45-54
Author(s):  
Mada Triandala Sibero ◽  
Nunung Febriany Sitepu ◽  
Tao Zhou ◽  
Yasuhiro Igarashi
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Trichoderma Reesei ◽  
Crude Extract ◽  
Antibacterial Agents ◽  
Ethyl Acetate Extract ◽  
Inhibition Zone ◽  
E Coli ◽  
Mycelial Extract ◽  
Fractionation Method

Bioguided fractionation method is commonly used to obtained targeted fraction with certain biological activity. In this study, bioguided fractionation method using HPLC was applied to obtained antibacterial fractions from marine-derived fungus Trichoderma reesei PDSP 5.7. The result shows that fraction from mycelium and medium extract had antibacterial activity against ESBL E. coli and S. enterica ser. Typhi with a range of inhibition zone was 1.35±0.15 to 8.82±0.22 mm2. From 32 fractions of each extract, the mycelial extract had 7 active fractions, 3 active fractions from broth medium which extracted using 1-butanol and 5 active fractions from ethyl acetate extract. This study indicated that crude extract of fungus T. reesei PDSP 5.7 was more potential as the source of antibacterial agents rather than the crude extract that obtained from its broth medium.

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.

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