Biological Evaluation of Synthesized Naringenin Derivatives as Antimicrobial Agents

2020 ◽  
Vol 18 ◽  
Author(s):  
Yogesh Murti
Keyword(s):  
Antimicrobial Activity ◽  
Phenyl Ring ◽  
Antimicrobial Agents ◽  
Plant Secondary Metabolites ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Agar Disc ◽  
Phenyl Rings ◽  
Grinding Technique

Abstract: Flavonoids are among the most abundant plant secondary metabolites and have been shown to have natural abilities as microbial deterrents and anti-infection agents in plants. Naringenin as one of the flavonoids and its derivatives have been reported to exhibit antimicrobial activity. The aim of the study was to evaluate synthesized novel naringenin derivatives (ND-1 to ND-12) substituted at 3-position with bulky substituent by using the grinding technique (Claisen-Schmidt reaction) as antimicrobial agents. Synthesized naringenin derivatives were evaluated for in-vitro antimicrobial activity by "Agar disc diffusion method". Novel naringenin derivatives showed mild to moderate antimicrobial activity with respect to standard drugs against two gram-positive, two gram-negative bacteria and two fungal strains. The substitution of naringenin derivatives at position 3 with substituted phenyl rings showed variation in activity as chloro, nitro and hydroxyl-substituted phenyl ring showed potent activity while methoxy substituted phenyl ring impede the activity. In conclusion, on the basis of the above findings, the substituted naringenin scaffolds may be selected as a skeleton for the development of flavonoid structurally-related compounds having antimicrobial activity

scholarly journals IN VITRO SCREENING OF ANTIMICROBIAL ACTIVITY OF ETHANOLIC EXTRACT OBTAINED FROM FICUS LYRATA WARB. (MORACEAE) LEAVES

2016 ◽  
Author(s):  
H. Tkachenko ◽  
L. Buyun ◽  
Z. Osadovskyy ◽  
M. Truhan ◽  
Ye. Sosnowski ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Ethanolic Extract ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Traditional Use ◽  
Agar Disc ◽  
Ficus Lyrata

In the current investigation, screening of ethanolic extract obtained from Ficus lyrata leaves against pathogenic bacteria has been done in order to assess the antimicrobial activity aimed at detecting new sources of antimicrobial agents. The antimicrobial activity of the extract was determined using agar disc diffusion method. The antibacterial activity of leaf extract of F. lyrata was tested against human pathogenic bacteria — both Gram-positive (Staphylococcus aureus, methicillin-resistant S. aureus and Streptococcus pneumoniae) and Gram-negative strains (Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli). The results of this study provide evidence that the ethanolic extract of F. lyrata leaves has a mild antimicrobial activities, apparently, attributed to the presence of various secondary metabolites, which confirm the traditional use of this plant for the treatment of diseases caused by pathogens. These data allow us to suggest that the extracts of F. lyrata can be used to discover antibacterial substances for developing new pharmaceuticals to control clinically important pathogens responsible for severe disorders.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

scholarly journals In vitro antibacterial effect of Euterpe oleracea Mart. and Theobroma grandiflorum hydroalcoholic extracts

2016 ◽  
Vol 21 (2) ◽  
Author(s):  
Lew Kan Sprenger ◽  
Elane Guerreiro Giese ◽  
Jeannie Nascimento Dos Santos ◽  
Marcelo Beltrão Molento
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Concentration ◽  
Antimicrobial Treatment ◽  
Significant Inhibition ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Euterpe Oleracea ◽  
Agar Disc ◽  
Euterpe Oleracea Mart

This study evaluated the in vitro antimicrobial activity of these species against strains of Gram-positive and Gram-negative bacteria. The hydroalcoholic extracts were prepared from dried leaves, pulp and seeds of E. oleracea Mart. and T. grandiflorum by continuous percolation with 70% ethyl alcohol. The antimicrobial activity was evaluated against four microorganisms by the agar disc diffusion method and the minimal inhibitory concentration (MIC) assay. The antimicrobial activity showed that the açai pulp and seeds possessed significant inhibition in Clostridium perfringens (320 and 640 MIC), Staphylococcus aureus (80 and 320 MIC) and Pseudomonas aeruginosa (640 and 2560 MIC). Cupuassu extracts showed no effect on any bacteria. The use of açai extract products can be a sustainable, viable and an accessible alternative for antimicrobial treatment. New studies should be conducted to determine better results for acai herbals and new formulations of cupuassu extracts.

scholarly journals Anti-microbial activity of heterocyclic cationic surface-active substances

2020 ◽  
Vol 24 (1) ◽  
pp. 36-40
Author(s):  
V. V. Pantyo ◽  
M. M. Fizer ◽  
O. I. Fizer ◽  
G. M. Koval ◽  
E.M. Danko
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Pathogenic Microorganisms ◽  
Disk Diffusion Method ◽  
E Coli ◽  
Quantitative Studies ◽  
Ionic Associates ◽  
Surface Active

Annotation. The development and rapid pace of the spread of resistance to antimicrobial agents predetermines the search for new methods of counteracting pathogenic and conditionally pathogenic microorganisms. In this context, studies of the antimicrobial activity of newly synthesized chemicals, which in the future can be considered as candidates for antiseptic and disinfectants, are relevant. The aim of the work was to determine the antimicrobial activity of new ionic associates based on the surface-active cetylpyridinium cation with respect to certain opportunistic microorganisms. The antimicrobial activity of four ionic associates based on the cetylpyridinium cation with respect to clinical isolates of E. coli, P. vulgaris, K. pneumonia, P. aeruginosa, S. aureus, as well as the collection test strains of S. aureus ATCC 25923, E. coli ATCC 29522 and P. aeruginosa ATCC 27853 was studied. Screening studies were performed by the disk diffusion method. With substances that showed an antimicrobial effect, quantitative studies were carried out by the method of serial macro-dilutions in a liquid nutrient media. Screening studies revealed the antibacterial activity of the substances against E. coli ATCC 25923, E. coli (clinical isolate), P. vulgaris and K. pneumonia. With these microorganisms quantitative studies were carried out with the determination of the minimum inhibitory and minimum bactericidal concentrations. The most pronounced antimicrobial activity for the investigated microflora was shown by tetraphenylborate and cetylpyridinium perchlorate. The MIC and MBC values of these substances ranged between 1.625–3.125 mmol / L and 3.125–12.5 mmol / L, respectively. The studied associates showed high antimicrobial activity against representatives of the Enterobacteriaceae family in in vitro studies. Promising is the further study of the effect of the counter-anion associates of cationic surfactants on the biofilm formation of conditionally pathogenic microorganisms.

Synthesis, Antimicrobial Evaluation and Molecular Docking of Some Potential 2,6-disubstituted 1H-Benzimidazoles; Non-Classical Antifolates

2019 ◽  
Vol 15 (7) ◽  
pp. 813-832 ◽  
Author(s):  
Sunil Harer ◽  
Manish Bhatia ◽  
Vikram Kawade
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Antimicrobial Agents ◽  
Cross Reactivity ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
One Pot ◽  
Disk Diffusion Method ◽  
Antimicrobial Evaluation

Background: Dihydrofolate reductase is one of the important enzymes for thymidylate and purine synthesis in micro-organisms. A large number of drugs have been designed to inhibit microbial DHFR but over the period of time, some drugs have developed resistance and cross reactivity towards the enzyme. Over the past few decades, benzimidazoles, triazoles and their derivatives have been grabbing the attention of the synthetic chemists for their wide gamut of antibacterial and antifungal activities targeting microbial protein DHFR. Objective: Our goal behind present investigation is to explore benzimidazoles class of drugs as microbial DHFR inhibitors by studying ligand-receptor binding interactions, in vitro enzyme inhibition assay and confirmation of anti-microbial activity against selected pathogenic microorganisms. Methods: A library containing thirty novel 2,6-disubstituted 1H-benzimidazoles was synthesized by one pot condensation of o-nitro aniline or 2,4-dinitro aniline with series of aldehydes or acetophenones using Na2S2O4 or SnCl2 respectively and reflux for 5-6hr. Structures of compounds have been confirmed by spectroscopic methods as 1H and 13C NMR, FT-IR and MS. In vitro DHFR inhibition study was performed by using Epoch microplate reader and IC50 of the test compounds was compared with Trimethoprim. In vitro antimicrobial activity was performed against selected clinical pathogens by agar disk diffusion method and MIC (µg/mL) was reported. Results: Moderate to good level of DHFR inhibition was observed with IC50 values in the range of 7-23 µM. Compounds B1, B19, B22, B24 and B30 expressed 1.1 to 1.4 folds more prominent DHFR inhibitory activity as compared to standard Trimethoprim. Remarkable antimicrobial activity was exhibited by B1, B19, B22, B24 and B30. Molecular docking study revealed perfect binding of test ligands with key amino acids of DHFR as Phe31, Ile94, Ile5, Asp27, Gln32 and Phe36. Conclusion: Nature of 1H-benzimidazole substituents at position 2 and 6 had influence over magnitude and type of molecular binding and variation in the biological activity. The present series of 1H-benzimidazoles could be considered promising broad-spectrum antimicrobial candidates that deserve in future for preclinical antimicrobial evaluation and development of newer antimicrobial agents targeting microbial DHFR.

scholarly journals In-vitro antimicrobial activity of different toothpastes

2018 ◽  
Vol 6 (2) ◽  
pp. 52-58
Author(s):  
Bikram Gautam ◽  
Elisa Dongol ◽  
Anima Shrestha
Keyword(s):  
Antimicrobial Activity ◽  
Oral Hygiene ◽  
Antimicrobial Agents ◽  
Active Agent ◽  
Antimicrobial Effect ◽  
Diffusion Method ◽  
Dilution Method ◽  
Wide Range ◽  
Test Organisms

Background: Tooth brushing with toothpaste is the most widely practiced form of oral hygiene. Toothpaste aids to improve oral hygiene and effective plaque removal. A wide range of chemicals, mainly antimicrobial agents, have been added to toothpastes which kill microorganisms by disrupting their cell walls and inhibiting their enzymatic activity.Objectives: The aim of the study was to determine the antimicrobial activity of toothpastes.Methods: Eight (Two herbal and six regular) toothpastes were selected for the study. The study was conducted from October to November 2016 at St. Xavier’s College’s microbiology laboratory. Antimicrobial activity of toothpastes were assessed by measuring inhibition zones by broth dilution method and agar well diffusion method.Results: Minimum Inhibitory Concentration determination by tube dilution method and cup well diffusion method was found to be same. The antimicrobial activity on test organisms was shown by all toothpastes (TH1, TH2, TR3, TR4, TR5, TR6, TR7 and TR8). Antimicrobial activity of all toothpastes were almost the same and was statistically significant (t>0.05)Conclusion: All eight toothpastes aids in lower microbial load. However, no toothpaste showed bactericidal and fungicidal effect against the tested microbes. The toothpaste containing only natural active ingredients were found to be more effective than the toothpaste containing chemical active agent followed by weaker antimicrobial effect given by the toothpaste containing both natural and chemical active ingredient as an antimicrobial agent.

1,5-Benzodiazepine derivatives as potential antimicrobial agents: design, synthesis, biological evaluation, and structure–activity relationships

2015 ◽  
Vol 13 (19) ◽  
pp. 5497-5509 ◽  
Author(s):  
Lan-Zhi Wang ◽  
Xiao-Qing Li ◽  
Ying-Shuang An
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Benzodiazepine Derivatives

36 novel 1,5-benzodiazepine derivatives were synthesized and evaluated for their in vitro antimicrobial activity. The results revealed that most of the 1,5-benzodiazepine derivatives exhibited considerable potency against all of the tested strains.

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 EVALUATION OF POTENTIAL ANTIMICROBIAL ACTIVITY OF SYNTHETIC FLAVONOIDS

2021 ◽  
Vol 10 (1) ◽  
pp. 76-82
Author(s):  
Prabhulingayya S Bhixavatimath ◽  
Yasmeen Maniyar ◽  
Akram Naikawadi ◽  
Vijayakumar D
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Oxidative Cyclization ◽  
In Vivo Studies ◽  
Diffusion Method ◽  
Flavonoid Compounds ◽  
Antibacterial And Antifungal

Introduction: In recent times, most of the currently available antimicrobial agents have developed resistance. Extensive pharmacological activities including bactericidal and bacteriostatic nature of flavonoids, made them as priority agents in this aspect of research study. Synthetic flavonoids such as hydroxy thiophen derivatives were considered to evaluate for antimicrobial activity in this study.   Objective: The present study involves the analysis for antimicrobial activity of thiophen substituted synthetic flavonoids. Methods: Claisen-Schmidt method of condensation fallowed by oxidative cyclization reactions from substituted hydroxyacetophenone with aromatic aldehydes were used to synthesize the various analogues of flavonoid compounds. Then these compounds after their FTIR, 1H NMR, MS spectral characterization and elemental analysis, were screened for in vitro antibacterial and antifungal activity by using disc diffusion method followed by determining their respective zone of inhibitions. Results: All the synthesized test flavonoid compounds exhibited the good antibacterial and antifungal  spectrum activity over B. subtilis, S. aureus, E. coli and P. aeurugenosa bacteria and Candida albicans and Aspergillus niger fungal microbes. However compounds such as F1, F2 and F4 showed moderately significant antibacterial activity against P. aerugenosa organism than the other test compounds and the same F1 and F2 test compounds exhibited significant antifungal activity at100µg concentration. Conclusion:  The present study demonstrated that the novel thiophen substituted flavonoids (F1, F2, F3 and F4 ) found to have promising antimicrobial and antifungal activity which needs to be confirmed by in vivo studies.

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