scholarly journals Facile Synthesis, Characterization and in vitro Antibacterial Efficacy of Functionalized 2-Substituted Benzimidazole Motifs

2019 ◽  
Vol 20 (1) ◽  
pp. 72
Author(s):  
Olayinka Oyewale Ajani ◽  
Olaoluwasubomi Eneyeme Joseph ◽  
King Tamunodikibugerere Iyaye ◽  
Natasha October ◽  
Damilola Victoria Aderohunmu ◽  
...  

A series of functionalized 2-substituted benzimidazole motifs was designed and successfully synthesized via thermal cyclization of 1,2-diaminobenzene on COOH end of L- leucine to achieve benzimidazole derivatives 6 as the essential precursor. The coupling of the precursor 6 with benzaldehyde derivatives a-h, ketone series i-k, and aryl sulfonyl chlorides l-n led to the formation of the targeted 2-substituted benzimidazole motifs 7a-n in improved yields. The targeted benzimidazole motifs were structurally authenticated through their spectral data and microanalytical parameters. The targeted final moieties were investigated for potential antimicrobial activity using the agar diffusion method with gentamicin as the clinical standard. All the compounds had a broad spectrum of activity with compound 7k having the highest remarkable activity with MIC of 0.98 ± 0.02 µg/mL and MBC value of 3.91 ± 0.10 µg/mL. These findings suggest that compound 7k containing camphor might be a good candidate for the design of new antimicrobial small-molecule drugs.

Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb

<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>


2002 ◽  
Vol 13 (3) ◽  
pp. 155-161 ◽  
Author(s):  
Brenda Paula Figueiredo de Almeida Gomes ◽  
Caio Cezar Randi Ferraz ◽  
Morgana Eli Vianna ◽  
Pedro Luiz Rosalen ◽  
Alexandre Augusto Zaia ◽  
...  

The aim of this study was to investigate in vitro the antimicrobial activity of calcium hydroxide in combination with several vehicles against some microorganisms commonly isolated from root canals. Antimicrobial activity was determined by the agar diffusion method. Stainless-steel cylinders were placed on each inoculated agar medium. The test medicaments and their controls were placed inside the cylinders. The zones of growth inhibition were measured and recorded after incubation for each plate and the results were analyzed statistically (ANOVA). The in vitro antimicrobial effects of the medications were ranked from strongest to weakest as follows: Ca(OH)2 + CMCP + glycerine, Ca(OH)2 + CMCP, Ca(OH)2 + glycerine, Ca(OH)2 + anesthetic, Ca(OH)2 + saline, Ca(OH)2 + H2O, Ca(OH)2 + polyethyleneglycol. The pastes with oily vehicles showed significantly larger mean zones of inhibition compared to those with aqueous or viscous vehicles. It was concluded that diffusion and antimicrobial activity of calcium hydroxide were affected by the type of vehicle used.


2014 ◽  
Vol 1060 ◽  
pp. 223-226
Author(s):  
Perayot Pamonsinlapatham

Moringa oleiferaLamk (Moringaceae) is a worldwide use for food and traditional medicine. In this study, plants were separated into seven parts: 1) Leaf, 2) Drum, 3) Branching, 4) Seed, 5) Outer stem, 6) Stem bark, and 7) Root, respectively. Then, they were extracted by two different methods: methanol soxhlet extraction and ethanol maceration. All crude extracts were tested for anti-bacterial activity by agar diffusion method and colorimetric micro-dilution plate technique. The results showed that 7 parts of Moringa crude extracts had low anti-bacterial activity againstStaphylococcus aureus,Escherichia coli, andPseudomonas aeruginosawhen compared with standard antibiotic (ampicillin or gentamycin). In conclusion, anti-bacterial effects ofM. oleiferacrude extracts had low anti-bacterial activityin vitrotest.


2012 ◽  
Vol 56 (8) ◽  
pp. 4500-4503 ◽  
Author(s):  
Virginie Planche ◽  
Sebastien Ducroz ◽  
Alexandre Alanio ◽  
Marie-Elisabeth Bougnoux ◽  
Olivier Lortholary ◽  
...  

ABSTRACTIn vitrointeraction of anidulafungin with voriconazole was tested by a microdilution broth checkerboard technique and an agar diffusion method against 30Aspergillusclinical isolates belonging to five different species. By using a complete inhibition endpoint, indifferent interactions were observed for 97% of the isolates by the checkerboard technique (FIC index from 0.5 to 2) and for 100% of the isolates by the agar diffusion method (variation of −2 to +1 log2dilutions).


Author(s):  
Megha Shukla ◽  
Sumeet Kaur Bhatia ◽  
Balbir Kaur

This research article describes the synthesis of phenyl hydrazone derivatives of 5-acetyl-6-methyl-4-substituted phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidines, as no derivatization has been reported at carbonyl functionality at position 5 of corresponding rings till date. The prepared derivatives were characterised using modern spectral techniques and were screened for their in-vitro anti-microbial activities by agar diffusion method. Among synthesised derivatives [II(a-g)], compound II(f) was found to be the most potent anti-bacterial agent and rest of the compounds had shown moderate to weak anti-bacterial activity.


2013 ◽  
Vol 3 (3) ◽  
pp. 117-120 ◽  
Author(s):  
Hina Sheth ◽  
Uday Kamath ◽  
Sai Ramesh ◽  
Keshav Singla

ABSTRACT Background and objectives Among the bacterial species which most often cause endodontic failure, Enterococcus faecalis is the most important. This study compared the antibacterial efficacy of tea tree oil with 3% sodium hypochlorite and 2% chlorhexidine as a root canal irrigant, against E. faecalis Materials and Methods Normal saline, tea tree oil, 3% sodium hypochlorite, 2% chlorhexidine and fresh stains of E. faecalis were used. Four round wells, 4 mm deep and 8 mm diameter, were punched using sterile cork borer in blood agar plates and divided into four groups: group A: normal saline (control), group B: 3% sodium hypochlorite, group C: 2% chlorhexidine and group D: tea tree oil. Agar well diffusion method was performed to compare the antibacterial efficacy of tea tree oil, 3% sodium hypochlorite and 2% chlorhexidine. Results The results were tabulated and statistically analyzed using analysis of variance (ANOVA). Tea tree oil showed comparable inhibition of bacterial growth with sodium hypochlorite and chlorhexidine. No zone of inhibition was shown by normal saline (control). Interpretation and conclusion Tea tree oil showed statistically significant antimicrobial activity against Enterococcus faecalis, which is very much similar to sodium hypochlorite and chlorhexidine. Abbreviations CHX: Chlorhexidine; E. faecalis: Enterococcus faecalis; NaOCl: Sodium hypochlorite. How to cite this article Kamath U, Sheth H, Ramesh S, Singla K. Comparison of the Antibacterial Efficacy of Tea Tree Oil with 3% Sodium Hypochlorite and 2% Chlorhexidine against E. faecalis: An in vitro Study. J Contemp Dent 2013; 3(3):117-120.


2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Dheeban Shankar P ◽  
Basker S ◽  
Karthik K ◽  
Karthik S

<p><strong>Activated carbon (AC) has found its attention in pollution control and wastewater treatment to remove various pollutants. Activated carbon can be prepared by physical and chemical activation methods. The chemical activation methods were advantageous over physical activation due to process accomplishment at lower temperature and greater yield which avoids burn-off char. Activated carbon was usually used as an adsorbent for dye removal from wastewater which could be related to their extended surface area, high adsorption capacity, microporous structure and special surface reactivity. Microbial pollution and contamination have produced various problems in industrial and medical fields. Based on this, the present study was attempted on the preparation of activated carbon from <em>Passiflora foetida</em> and evaluating for its antibacterial efficacy against twelve different microorganisms by agar well diffusion method. The results were found to be very effective with higher zone of inhibition against almost all the microorganisms tested. Moreover, the activity was considerably more against <em>Shigella flexneri (MTCC 1457) </em>and <em>Klebsiella pneumoniae (MTCC 10309).</em>In addition to this, the shake flask test in saline had proved that the colonial growth of <em>E.coli</em> was inhibited with respect to the concentration of activated carbon and time of incubation.</strong></p><p><strong> </strong></p>


Author(s):  
Pavla Sládková ◽  
Eva Rejchrtová ◽  
Tomáš Komprda ◽  
Doubravka Rožnovská

The aim of this work was to test in vitro the ability of the components in the spice mix usually used for the production of the „paprikáš“ sausage (P) to inhibit the growth of tyramine and histamine forming microorganisms. The ability of the P spice mix components to inhibit the growth of the Pediococcus pentosaceus and Enterococcus faecalis CNRZ 238 species was tested by the agar diffusion method. The tested cultures were chosen as positive to a gene sequence for tyrosindecarboxylase (tyrDC). None of the tested P spice components or the mix as a whole inhibited growth of Pediococcus pentosaceus and Enterococcus faecalis CNRZ 238.


2015 ◽  
Vol 8 (1) ◽  
pp. 64
Author(s):  
Marcos V.S. Silva ◽  
Tayara S. Frazão ◽  
Melyssa M.A.V. Ferreira ◽  
Jandir S. Sales ◽  
Denis B. Vieira ◽  
...  

<p class="Default">The <em>Psidium guajava L</em>. specie is a perennial shrub, belonging to the <em>Myrtaceae</em> family and it is popularly known as guava, its leaves are used in therapy for treating various diseases. The study aims to evaluate the antibacterial activity <em>in vitro </em>of manipulated product obtained from dried extract of the leaves of <em>P. guajava </em>L. front standard bacteria ATCC and clinical isolates. The tests were conducted on bacterial samples: <em>Staphylococcus aureus </em>(ATCC 25923), <em>Pseudomonas aeruginosa </em>(ATCC 27883), <em>Escherichia coli </em>(ATCC 25922), <em>Salmonella spp</em>, <em>Acinetobacter baumannii</em>, <em>Proteus mirabilis</em>, <em>Shigella flexneri</em>, <em>Staphylococcus epidermidis</em>, <em>Staphylococcus haemolyticus</em>, <em>Streptococcus agalactiae, Streptococcus mutans</em>. Among the tests can be mentioned phytochemical of the ethanol extract (EE), microbiological control and physical-chemical analysis of the product and microbiological tests such as agar diffusion method (wells), minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), an evaluation test of hemolytic capacity of the solution and in vitro assay cytotoxic activity were performed, . The best result of the product in the agar diffusion method was front <em>Staphylococcus epidermidis</em>, while the lower MIC and MBC were front <em>Staphylococcus aureus </em>(ATCC 25923). The product showed no hemolytic activity and no cytotoxic activity at the tested concentrations. According to the test results, it is believed on the possibility of the production of a pharmaceutical formulation derived from the dry extract of <em>Psidium guajava</em>, since it showed great antibacterial activity.</p>


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