Synthesis of N-mono- and N,N-dialkylated imidazole derivatives based on (adamantyl-1)bromomethylketone and study of their antibacterial activity

2020 ◽  
Vol 63 (7) ◽  
pp. 24-30
Author(s):  
Anton V. Basantcev ◽  
◽  
Andrey A. Danilin ◽  
Tatyana I. Vasileva ◽  
Petr P. Purygin ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Petroleum Industry ◽  
Antibiotic Sensitivity ◽  
Bactericidal Effect ◽  
Diffusion Method ◽  
Imidazole Derivatives ◽  
Antibacterial And Antifungal Activities ◽  
Sulfur Bacteria ◽  
Antibacterial And Antifungal ◽  
Counter Synthesis

Different methods for the synthesis of N-mono- and N,N-dialkylated imidazole derivatives represent certain interest not only for organic chemistry, but also for medicine. N-alkylated imidazoles are the basis of drugs with antibacterial and antifungal activities. This allows us to consider them as efficient synthons for the synthesis of modern medicines. The quaternary imidazolium salts are applied as anticorrosive substances in petroleum industry due to their antibacterial activity against sulfur bacteria. The introduction of (adamantoyl-1)methyl group with high lipophilicity to the composition of imidazole derivatives contributes in some cases to increasing their bactericidal effect. In this paper, N-mono- and N,N-dialkylation of imidazole derivatives was carried out by using (adamantyl-1)bromomethylketone. The newly obtained compounds were identified using 1H NMR and IR spectroscopy, and its homogeneity by TLC. In addition, the counter synthesis was conducted with previously obtained N-adamantoylmethylimidazoles to define the structure of quaternary salts. The experimental results demonstrated identical of 1,3-bis[(adamantoyl-1)methyl]imidazolium bromides which were received in two various ways. To determine antibacterial activity of received substances we were examined its influence on E.Coli cells. DMSO was used as a comparison control. The experiment was carried out in MPA medium. The disc-diffusion method was selected as a test of the antibiotic sensitivity of bacteria.

scholarly journals Evaluation of Antimicrobial Activity of Sida cordifolia Leaf Extract

2019 ◽  
pp. 1-7 ◽  
Author(s):  
Dhanapal Venkatachalam ◽  
Samuel Thavamani ◽  
Aneesh C. Sebastian ◽  
V. B. Anju ◽  
Christy Mathew ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Pathogenic Fungus ◽  
Chloroform Extract ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Sida Cordifolia ◽  
Antibacterial And Antifungal

Objective: The objective of the study was to evaluate in-vitro efficacy of antibacterial, and antifungal activities of chloroform extract of leaf of Sida cordifolia L. against some human pathogenic bacterial and fungal strains. S. cordifolia (Malvaceae) is used as anti-rheumatic, analgesic, antipyretic, anti-asthmatic, nasal decongestant, antiviral, laxative, diuretic, aphrodisiac, hypoglycemic, hepatoprotective and in the treatment of Parkinson disease. Methodology: Chloroform extract of S.cordifolia was used for antimicrobial screening. Antibacterial activity was tested against pathogenic bacterial strains Eschericha coli and Staphylococcus aureus. Also antifungal activity was tested against one human pathogenic fungal strain i.e. Candida albicans. Antibacterial and antifungal activities of S. cordifolia extract was carried out by using disc diffusion method. Results: Chloroform extract of S. cordifolia showed the largest zone of inhibition (10mm) against S. aureus at 50µgm/mL and no zone of inhibition against E.coli at 50µgm/ml. Chloroform extract has shown more potent antibacterial activity against S.aureus. Chloroform extract was found to be more effective against human pathogenic fungus C. albicuns. The zone of inhibition of chloroform extract was 10mm.The phytochemical screening demonstrated the presence of different types of compounds like alkaloids, tannins and phenolic compounds which may contribute for the anti-microbial action of this plant.  Conclusions: The results concludes that chloroform extract of S. cordifolia leaf possess antimicrobial activity.

scholarly journals Activity of Aristolochia bracteolata against Moraxella catarrhalis

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Malik Suliman Mohamed ◽  
Mona Timan Idriss ◽  
Amgad I. M. Khedr ◽  
Haidar Abd AlGadir ◽  
Satoshi Takeshita ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Moraxella Catarrhalis ◽  
Methanol Extract ◽  
Diffusion Method ◽  
Disk Diffusion Method ◽  
Antibacterial And Antifungal Activities ◽  
Bioassay Guided Fractionation ◽  
Test Organisms ◽  
Antibacterial And Antifungal ◽  
Aristolochia Bracteolata

A bioassay-guided fractionation of methanol extract of Aristolochia bracteolata whole plant was carried out in order to evaluate its antimicrobial activity and to identify the active compounds in this extract. Antibacterial and antifungal activities of methanol extract against gram-positive, gram-negative, and fungal strains were investigated by the agar disk diffusion method. Among the strains tested, Moraxella catarrhalis and sea urchin-derived Bacillus sp. showed the highest sensitivity towards the methanol extract and hence they are used as test organisms for the bioassay-guided fractionation. From this extract, aristolochic acid 1 (AA-1) has been isolated and has showed the greatest antibacterial activity against both standard strain and clinical isolates of Moraxella catarrhalis with equal minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 25 and 50 μg/mL. Modification of the AA-1 to AA-1 methyl ester completely abolished the antibacterial activity of the compound and the piperonylic acid moiety of AA-1 which suggested that the coexistence of phenanthrene ring and free carboxylic acid is essential for AA-1 antibacterial activity.

Synthesis and Evaluation of Demethoxyviridin Derivatives as Potential Antimicrobials

2005 ◽  
Vol 60 (9-10) ◽  
pp. 686-692
Author(s):  
Ismail Kiran ◽  
Semra Ilhan ◽  
Tamer Akar ◽  
Lacine Tur ◽  
Erdinc Erol
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Geotrichum Candidum ◽  
Diffusion Method ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Antibacterial And Antifungal Activities ◽  
Agar Dilution ◽  
Antibacterial And Antifungal

Abstract The in vitro antibacterial and antifungal activities of demethoxyviridin and some synthetic analogues were evaluated by the agar diffusion method. The minimum inhibitory concentrations (MIC) of the active compounds were also determined by the agar dilution method. Demethoxyviridin (1) showed moderate antibacterial activity against most of the strains tested. 1α-Hydroxydemethoxyviridin (3) showed antibacterial activity and the most potent in vitro antifungal activity with MIC of 20 μg/ml (0.062 mm) against Aspergillus niger, A. fumigatus, A. flavus, A. parasiticus, Fusarium solani, F. graminarum, Geotrichum candidum whereas 5′-methylfuro-(4′,3′,2′-4,5,6)androst-5-ene-3,17-dione (7) exhibited very weak antifungal activity against Candida albicans only.

scholarly journals Antibiotic sensitivity and in vitro antimicrobial activity of plant extracts to pseudomonas fluorescens isolates collected from diseased fish

1970 ◽  
Vol 1 (4) ◽  
pp. 82-88 ◽  
Author(s):  
MJ Foysal ◽  
MM Rahman ◽  
M Alam
Keyword(s):  
Antibacterial Activity ◽  
Pseudomonas Fluorescens ◽  
Plant Extracts ◽  
Antibiotic Sensitivity ◽  
Diffusion Method ◽  
Biochemical Tests ◽  
Leaf Extracts ◽  
Sensitivity Pattern ◽  
Medicinal Plant Extracts

Studies were conducted to identify Pseudomonas fluorescens isolates from a collection of bacteria isolated from bacterial haemorrhagic septicaemia infected carp and catfish, evaluate their antibiotic sensitivity pattern and screen the antibacterial activity of some medicinal plant extracts against the isolates.. A total of 10 isolates were identified as P. fluorescens by morphological, physiological and biochemical tests. In vitro antibiotic sensitivity test of the P. fluorescens isolates were conducted by disc diffusion method for seven antibiotics where, all of the isolates were found to be sensitive only against streptomycin and gentamycin but, most of the isolates (80%) were found resistant to chloramphenicol (C). Moreover, eighty percent of the isolates showed resistance to multiple antibiotics. A total of 118 plant extracts were screened for their antibacterial activity against the P. fluorescens isolates where the isolates exhibited sensitivity to 30 samples. Leaf extracts of Tamarindus indicus, Terminalia chebula, Citrus aurantifolia, Eugenia caryophyllata and Spondias pinnata were found to inhibit the growth of all of the P. fluorescens isolates. DOI: http://dx.doi.org/10.3329/ijns.v1i4.9733 IJNS 2011 1(4): 82-88

Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Chemical Properties ◽  
Diffusion Method ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

scholarly journals Monomyristin and Monopalmitin Derivatives: Synthesis and Evaluation as Potential Antibacterial and Antifungal Agents

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3141 ◽  
Author(s):  
Jumina ◽  
Asma Nurmala ◽  
Anggit Fitria ◽  
Deni Pranowo ◽  
Eti Sholikhah ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Positive Control ◽  
Antifungal Activities ◽  
Amberlyst 15 ◽  
Antibacterial And Antifungal Activities ◽  
High Antibacterial Activity ◽  
Carbon Chains ◽  
Acyl Position ◽  
Antibacterial And Antifungal ◽  
Isopropylidene Glycerol

In the present work, monoacylglycerol derivatives, i.e., 1-monomyristin, 2-monomyristin, and 2-monopalmitin were successfully prepared from commercially available myristic acid and palmitic acid. The 1-monomyristin compound was prepared through a transesterification reaction between ethyl myristate and 1,2-O-isopropylidene glycerol, which was obtained from the protection of glycerol with acetone, then followed by deprotection using Amberlyst-15. On the other hand, 2-monoacylglycerol derivatives were prepared through enzymatic hydrolysis of triglycerides in the presence of Thermomyces lanuginosa lipase enzymes. The synthesized products were analyzed using fourier transform infrared (FTIR) spectrophotometer, gas or liquid chromatography-mass spectrometer (GC-MS or LC-MS), and proton and carbon nuclear magnetic resonance (1H- and 13C-NMR) spectrometers. It was found that monomyristin showed high antibacterial and antifungal activities, while 2-monopalmitin did not show any activity at all. The 1-monomyristin compound showed higher antibacterial activity against Staphylococcus aureus and Aggregatibacter actinomycetemcomitans and also higher antifungal activity against Candida albicans compared to the positive control. Meanwhile, 2-monomyristin showed high antibacterial activity against Escherichia coli. The effect of the acyl position and carbon chains towards antibacterial and antifungal activities was discussed.

scholarly journals Phytochemical investigation and in vitro antimicrobial activity of Richardia scabra

2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi
Keyword(s):  
Antimicrobial Activity ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Weed Species ◽  
Antibacterial And Antifungal Activities ◽  
Agar Plug ◽  
Phytochemical Investigation ◽  
Antibacterial And Antifungal ◽  
Simple Sugar

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>

scholarly journals ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY OF SILVER NANOPARTICLES AGAINST NEISSERIA GONORRHOEAE AND CANDIDA ALBICANS

2020 ◽  
Vol 8 (6) ◽  
pp. 179-187
Author(s):  
Titik Taufikurohmah ◽  
Tasha Anandya Tantyani
Keyword(s):  
Antibacterial Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Neisseria Gonorrhoeae ◽  
Diffusion Method ◽  
Antibacterial And Antifungal Activity ◽  
Disk Diffusion Method ◽  
Fungal Inhibition ◽  
Inhibition Response ◽  
Antibacterial And Antifungal

This Research on the antibacterial and antifungal activity of nanosilver against Neisseria gonorrhoeae and Candida albincas fungi has been carried out. The purpose of this study was to determine antibacterial activity of nanosilver against Neisseria gonorrhoeae and antifungal activity against Candida albincas. Synthesis Nanosilver uses bottom up method and characterized using UV-Vis Spectrophotometer. Nanosliver concentrations used were 30, 40, 50, and 60 ppm. Antibacterial and antifungal activity tests using disk diffusion method. Observations obtained in form of the presence or absence of clear zones formed around paper discs indicate the inhibition of nanosilver on microbial growth. The results of testing the antifungal activity of Candida albicans on nanosilver with concentrations of 30, 40, 50 and 60 ppm resulted in clear zones of 9.73 nm, 11.46 nm, 11.93 nm, and 13 nm with fungal inhibition response categories is medium and strong. The results antibacterial activity test of Neisseria gonorrhoeae on nanosilver with concentrations of 30, 40, 50 and 60 ppm did not show any clear zone around the disc, it showed that nanosilver in this study did not have antibacterial activity against Neisseria gonorrhoeae.

Antibacterial Effect of Disinfectants and Antiseptics

2021 ◽  
Vol 6 ◽  
pp. 47-62
Author(s):  
Nikoleta Hristova ◽  
Margarita Tzenova ◽  
Martina Ivanova ◽  
Emilia Grozdanova ◽  
Slavena Davidova ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bactericidal Effect ◽  
Diffusion Method ◽  
Ethacridine Lactate ◽  
Synthetic Agents ◽  
Morphological Differences ◽  
Zero Effect ◽  
Almost All ◽  
Antibacterial And Antifungal ◽  
Strain Ofescherichia Coli

Disinfectants and antiseptics are substances or solvents which play a key role inthe control of infections. Their wide functionality is applied in almost all human activities. Theseagents can have antiviral, antibacterial and antifungal effects. Disinfectants are synthetic agents thebiocidal effect of which destroys microorganisms in the environment, while antiseptics are appliedlocally, primarily on skin and/or mucosae. The morphological differences between Gram (+) andGram (–) bacteria raise questions regarding the biocidal effects of antibacterial agents againstdifferent types of infectious agents. The aim of our study is to evaluate the biocidal effect ofdisinfectants and antiseptics available on the market. The study uses a reference strain ofEscherichia coli and a laboratory isolate of Staphylococcus aureus. The analysis was conductedusing the agar well diffusion method. Results show that sodium hypochlorite, hydrogen peroxideH2O2 and mouthwashing water demonstrate strong bactericidal effect on both Gram (+) and Gram(–) bacteria. The bath cleaner gel, which is considered effective against Escherichia coli,demonstrated effectiveness against Staphylococcus aureus instead. The dishwashing gel,ethacridine lactate, silver water and lavandula water show intermediate or zero effect againstEscherichia coli and Staphylococcus aureus.

scholarly journals Studies on Antibacterial and Antifungal Activities and Minimum Inhibitory Concentrations of Mixed Ligand Transition Metal Complexes of Dibasic Acids as Primary and Heterocyclic Bases as Secondary Ligands

1970 ◽  
Vol 46 (3) ◽  
pp. 365-368 ◽  
Author(s):  
MA Akbor ◽  
MS Islam ◽  
N Akhter ◽  
S Ahmed ◽  
S Siraj
Keyword(s):  
Antifungal Activity ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Mixed Ligand ◽  
Diffusion Method ◽  
Antifungal Activities ◽  
Minimum Inhibitory Concentrations ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Mixed ligand (diphenic/ adipic as primary Ligand and quinoline / 8 - hydroxyquinoline as secondary) transition metal complexes of Cobalt (II), Cupper (II), Rhodium (III) and Platinum (IV) ions were synthesized and characterized. Their antibacterial activities against ten bacteria had been evaluated by the disc diffusion method,whilst their antifungal activities against two fungi had been also evaluated by the same method. Minimum inhibitory concentrations (MIC) had been evaluated against six bacteria. The MIC of the complexes against Shigella dysenteriae, Samonella typhi, Streptococcus-β-haemolyticus and Bacillus megaterium were 32 μg/ml; whilst Escherichia coli and Samonella typhi-A the MIC of Co (II) and Pt (IV) were 32μg/ml and those of Cu(II) and Rh(III) complexes were 64 μg/ml. It was found that Cobalt (II), Cupper (II) & Rhodium (III) complexes had pronounced antibacterial and antifungal activities. Platinum (IV) complex had moderate antibacterial and antifungal activity. These values indicate that these are active compounds. Key words: Mixed Ligand; Transition metal; Antimicrobial Activity; Antifungal Activity Minimum Inhibitory Concentrations (MIC) DOI: http://dx.doi.org/10.3329/bjsir.v46i3.9044 BJSIR 2011; 46(3): 365-368

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