scholarly journals SYNTHESIS, ANTIMICROBIAL, ANTITUBERCULAR AND CHEMINFORMATIC STUDIES OF 2-(1-BENZOFURAN-2-YL)-N'-[(3Z)-2-OXO-1, 2-DIHYDRO-3H-INDOL-3-YLIDENE] QUINOLINE-4-CARBOHYDRAZIDE AND ITS DERIVATIVES

2017 ◽  
Vol 9 (5) ◽  
pp. 260 ◽  
Author(s):  
S. Santoshkumar ◽  
N. D. Satyanarayana ◽  
R. Anantacharya ◽  
P. Sameer
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
In Silico ◽  
Antitubercular Activity ◽  
Mean Value ◽  
Diffusion Method ◽  
Pharmacokinetic Parameters ◽  
Moderate Activity ◽  
Significant Activity ◽  
Standard Drug

Objective: Synthesis of novel 2-(1-benzofuran-2-yl)-N'-[(3Z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene] quinoline-4-carbohydrazide and its derivatives for antimicrobial and antitubercular activity.Methods: Synthesis was carried out using the general method and the structures were confirmed by IR, 1H-NMR, [13]C-NMR and mass spectral analysis. The antibacterial activity was carried by agar well diffusion method, antifungal activity was performed by poison food technique and antitubercular activity was carried out by Microplate Alamar Blue Assay (MABA) method with the help of H37Rv. In silico absorption, distribution, metabolism, excretion, toxicity (ADMET) study of the drug, likeliness was carried out in ACD/lab-2.Results: The results revealed that at 25 mg/ml concentration, compounds 3a and 5a showed good antibacterial activity at 3.5±0.1, 3.8±0.3, 3.6±0.2 respectively against E. coli, K. pneumonia and S. typhimurium, when compared with drug streptomycin with similar concentration. The percentage of inhibition found at 50 µg/ml concentration, compounds 2b and 6a exhibited good antifungal activity at 53±1.15, 57±1.52 against A. flavus and C. neoformans, compared with standard drug fluconazole. The increase in activity was found to be dose dependent. The analogue 2a showed good antitubercular activity at 12.5±0.5 µg/ml, compounds 2b, 3a, 4a-b, 5a-b and 6a-b exhibited significant activity at 25±0.57 µg/ml and compound 3b showed moderate activity at 50±0.57 µg/ml. The mean value of P<0.05 were considered to be statistically significant. The absorption, distribution, metabolism, excretion and toxicity studies of the entitled molecules were analyzed and found to be in acceptable range.Conclusion: The study reveals that compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics, suggesting to be potentially best inhibitor of H37Rv strain. The in silico ADME analysis also revealed that all the compounds were in acceptable range to obey the pharmacokinetic parameters.

SYNTHESIS AND EVALUATION OF SOME SUBSTITUTED 2-AMINOTHIAZOLE DERIVATIVES FOR THEIR ANTITUBERCULAR, ANTIMICROBIAL & ANTIFUNGAL ACTIVITY

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (01) ◽  
pp. 24-32
Author(s):  
S. R. Pattan ◽  
◽  
S. H Kale ◽  
R. A. Mali ◽  
S. S. Dengale ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Antitubercular Activity ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Standard Drug ◽  
E Coli ◽  
H Nmr ◽  
Antimicrobial And Antifungal Activity ◽  
Micro Organisms

Millions of people are affected by infectious diseases caused by micro-organisms. Further the widespread microbial resistance had renewed the interest in quest for new antitubercular, antimicrobial & antifungal agents. The present study deals with synthesis & evaluation of some substituted 2-aminothiazole derivatives for their antitubercular, antimicrobial and antifungal activity. 2-aminothiazole derivatives were synthesized by treating substituted acetophenones with thiourea in presence of bromine to give 2-amino 4-substituted phenylthizole and then further treated with chloracetyl chloride to give 2-chloro-N-(4-substituted phenylthizole-2-yl)-acetamide which on refluxing with primary amine gives 15 derivatives. All the synthesized compounds were characterized by IR, H-NMR and elemental analysis.All the synthesized compounds were screened for their antibacterial activity against S. aureus and E. coli by using cup plate agar diffusion method. The activity was measured in terms of zone of inhibition and compared with standard drug ciprofloxacin, sulfonamide. The aminothiazole derivatives were evaluated for antitubercular activity and their result were compared with standard streptomycin.

scholarly journals Antifungal Activity of Various Extracts of Seeds of the Plant Malva Parviflora (Linn)

2017 ◽  
Vol 14 (4) ◽  
pp. 1409-1412
Author(s):  
Jadhav Raina ◽  
Parihar Sangeeta
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antifungal Agent ◽  
Antifungal Agents ◽  
Diffusion Method ◽  
Dilution Method ◽  
Significant Activity ◽  
Water As Solvent ◽  
Malva Parviflora ◽  
Agar Well Diffusion Method

ABSTRACT: Development of more effective and less toxic antifungal agents is required for the treatment of various fungal disease.Plants and their extraction preparation have beenused as medicine against infectious diseases.The present study was aimed to study, the antifungal activity of the seeds of various seed abstract of plant Malva Parviflora (Linn). The antifungal activity of seeds extract of plant was determine by using agar well diffusion method,MIC(minimum inhibitoryconcentration) and MFC (minimum fungicidal count)by using micro dilution method . The seeds extract of the plant were examined using Methanol, Ethyl acetate ,Petroleum ether and water as solvent and tested against different fungi pathogens. From the result it can be concluded that the all the seeds extract shows the significant activity against the micro organism, hence these extract may be used as a source of antifungal agent obtained from herbal medicine and may be explore as new and effective antifungal agent. Various solvent extracts of the plant Malva parvifiora (Linn) have been found to possess enough antibacterial activity and may potentially be explored as human antifungal agent.

scholarly journals Screening of Antimicrobial Activity of Various Extracts of the Stem Justicia gendarussa

2019 ◽  
pp. 1-7
Author(s):  
Dhanapal Venkatachalam ◽  
Akhib Rahman ◽  
Basil Sunny ◽  
Jensy Jacob ◽  
Nikhil Kuriyan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Aqueous Extract ◽  
Antimicrobial Agents ◽  
Pathogenic Fungus ◽  
Hexane Extract ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Standard Drug ◽  
Antibacterial And Antifungal

Objective: The present study was designed to check in-vitro efficacy of Antibacterial and antifungal activity of aqueous and hexane extracts of stem of Justicia gendarussa against selected bacterial and fungal strains. Justicia gendarussa, belonging to the family Acanthaceae, commonly known as ‘‘vatham kolli’ was used in treatment of bronchitis, inflammation, eye diseases, ear ache, vaginal discharges, rheumatism, dysentery, eczema and jaundice. Methodology: Hexane and aqueous extracts of Justicia gendarussa 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 Justicia gendarussa extract was carried out by using disc diffusion method. Results: Aqueous extract of Justicia gendarussa showed the largest zone of inhibition (5mm) against Eschericha coli, at 50µgm/ml and 3mmzone of inhibition against S. aures, at 50µgm/ml. Hexane extract does not   showing activity against to human pathogenic E. coli and S. aures, at 50µgm/ml. Aqueous extract has shown more potent antibacterial activity against Eschericha coli. Aqueous extract was found to be more effective against human pathogenic fungus Candida albicuns than hexane extract and standard drug. The zone of inhibition of Aqueous extract was 11mm and the zone of inhibition of hexane extract was7mm and standard only 2mm.The phytochemical screening demonstrated the presence of different types of compounds like terpenoids, tannins, and flavonoids which may contribute for the anti-microbial action of this plant. Conclusions: These findings provide scientific evidence of traditional use of Justicia gendarussa and also indicate the potential of this plant for the development of antimicrobial agents.

scholarly journals Synthesis of some novel 1H-indole derivatives with antibacterial activity and antifungal activity

2020 ◽  
Vol 9 (2) ◽  
pp. 961-967 ◽  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Indole Derivatives ◽  
Standard Drug ◽  
Paper Disk ◽  
Standard Medication ◽  
Tube Dilution

The present research works a series of new 1H-Indole derivatives were synthesized. The title compound was obtained by the reaction of indole with chloroacetylchloride in toluene afforded 2-chloro-1-(indoline-1-yl) ethanone which reacts with 1,4 diamine benzene in chloroform afforded 2-((4-aminophenyl)amino)-1-(1H-indol-1-yl)ethan-1-one, on further reaction with various acetophenone in presence of acetic acid in ethanol gave various final derivatives. After synthesis of compounds, the synthesized compounds were characterized by their IR, 1HNMR spectral data and elemental analysis. These derivatives were screened for their antimicrobial activity (Paper-disk-plate technique (disc diffusion method) and Tube-dilution technique (broth microdilution technique), antifungal activity of all synthesized compounds were evaluated against Aspergillus niger and Candida albicans (ATCC 10231) using Fluconazole as the standard drug using the paper plate method and antibacterial activity against both Gram-positive (Bacillus subtilis) and Gram-negative bacteria (Escherichia coli) using Ampicillin as standard medication at a concentration of 50g/ml, 100g/ml. The collected compounds were evaluated for antibacterial activity and antifungal activity. All compounds exhibit significant antimicrobial activity.

scholarly journals Antifungal activity in the methanolic, aqueous and hexane extracts of Capparis deciduas

2018 ◽  
Vol 16 ◽  
pp. 205873921878170
Author(s):  
Shaista Jameel ◽  
Saeed Ahmad ◽  
Muhammad Akram ◽  
Rida Zainab ◽  
Aamir Sharif
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Diffusion Method ◽  
Significant Activity ◽  
Aqueous Extracts ◽  
Standard Drug ◽  
Methanolic Extracts ◽  
Research Activities ◽  
Hexane Extracts ◽  
Bioactive Ingredients

The use of plants to cure specific ailments is as antique as human civilization. These days, in the modern era, there is a growing concern by public opinion regarding the use of synthetic medicine due to their side effects and cost. These facts led to the discovery of some economical and alternative drugs with fewer side-effects. In this study, methanolic, hexane and aqueous extracts of Capparis deciduas have been evaluated for their antifungal activity against medically important fungal strains – Candida albicans and Aspergillus niger using disc diffusion method at a dose of 1.8, 2.9, 6.5, 12.6, 25, 50 and 75 (µg/mL). Zone of inhibition for antifungal activity of these extracts was compared with that of a standard drug like fluconazole. The methanolic extracts of C. decidua showed significant activity against C. albicans (minimum inhibitory concentration (MIC): 1.8 µg/mL), for hexane extracts the MIC was 2.9 µg/mL and for aqueous extracts, no MIC can be observed. C. decidua did not show significant activity against A. niger. Our finding showed that C. decidua has antifungal activity and further phytochemical analyses of these plants should be carried out to determine the bioactive ingredients that may serve as a lead in the progress of novel research activities in the pharmaceuticals industry.

Synthesis and In Silico Molecular Docking Studies on Substituted Piperic Acid Derivatives as Inhibitors of Bacterial DNA Gyrase

2020 ◽  
Vol 16 (3) ◽  
pp. 281-294
Author(s):  
Bhawna Chopra ◽  
Ashwani K. Dhingra ◽  
Deo N. Prasad ◽  
Sakshi Bhardwaj ◽  
Sonal Dubey
Keyword(s):  
Antibacterial Activity ◽  
Molecular Docking ◽  
In Silico ◽  
Docking Studies ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Molecular Docking Studies ◽  
In Silico Molecular Docking ◽  
Electron Donating Groups

Background: Piperine or piperic acid was isolated from fruits of Piper nigrum and had been reported as pharmacological valuable bioactive constituents. Keeping in view, a series of piperic acid-based N heterocyclic’s derivatives were synthesized and evaluated for antibacterial activity. All these prepared ligands were docked to study the molecular interactions and binding affinities against the protein PDB ID: 5 CDP. Objective: To meet the real need of newer antibacterials, we designed and synthesized scaffolds with good antibacterial activity. The obtained antibacterials have been validated in terms of ligand-protein interaction and thus prove to build up as good drug candidates. Methods: Antibacterial activity of the compounds were carried out against bacterial strains; three Grampositive and three Gram-negative bacterial strains using agar well diffusion method. In silico molecular docking studies were carried out using Glide (grid-based ligand docking) program incorporated in the Schrödinger molecular modeling package by Maestro 11.0. Results: Compounds BC 28, BC 32, and BC 33 exhibits antibacterial activity along with Glide docking score of -8.580, -9.753 kcal/mol, and -8.813 kcal/mol, respectively. Docking studies explained hydrogen bonding, pi-pi, and hydrophobic interactions with amino acid residues which explain the binding affinity of the most docked ligand with protein. Conclusion: In the present study, substituted piperic acid was synthesized and evaluated as antibacterial compared with standard drug ciprofloxacin and results interpret that having nitrogen as heteroatom in the heterocyclic nucleus found to be more potent than the standard drug ciprofloxacin. On comparing, substitution with electron-donating groups generates excellent antibacterial potential against the bacterial strains. It was also proved that having substitution with electron-donating groups on meta and para position with triazoline ring system exhibits greater potential while compounds which have a meta- electron-donating substituent showed lesser activity with thiazole nucleus. In addition, structure-based activities of the prepared analogs were discussed under Structure-Activity Relationship (SAR) section.

scholarly journals Synthesis, in silico studies and antibacterial activity of some novel 2-substituted benzimidazole derivatives

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Ramakrishna Chintakunta ◽  
Geethavani Meka
Keyword(s):  
Antibacterial Activity ◽  
Melting Point ◽  
In Silico ◽  
Software Tool ◽  
Benzimidazole Derivatives ◽  
Recrystallization Process ◽  
Standard Drug ◽  
In Silico Studies ◽  
Drug Synthesis ◽  
Percentage Absorption

Abstract Background The o-phenylenediamine is a versatile starting material for several compounds. Synthesized o-phenylenediamine and amino acids (glycine, alanine, aspartic acid, and l-proline) undergo condensation via Phillips reaction. The synthesized compound showed the promising antibacterial activity of Bacillus subtilis and Pseudomonas aeruginosa at the concentration of 100, 50, 25, 12.5, 6.25, 3.12, 1.6, 0.8, 0.4, and 0.2 μg/ml. Ciprofloxacin was used as standard drug. Synthesis of benzimidazole derivatives was carried out and purified by recrystallization process using ethanol. Substituted derivatives were characterized by melting point, TLC and spectroscopic methods include FT-IR and 1H-NMR. Results In silico studies were adopted for synthetic derivatives by Molinspiration, ChemDraw, and online software tool. Minimum inhibitory concentration (MIC) values of B. subtilis and P. aeruginosa were reported, and benzimidazole ligands and Molinspiration scores were generated and listed. Conclusion The more negative values indicate a higher binding affinity. The generated ligand observations can be visualized. Physical constants of synthesized derivates such as solubility and melting point were determined. Bioactivity scores were noted for different derivatives and predicted percentage absorption in the gut. The antibacterial activity was performed using the MIC method (aerobic).

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 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.

scholarly journals A new group of compounds derived from 4-, 5-, 6- and 7-aminoindoles with antimicrobial activity

2018 ◽  
Vol 4 (3) ◽  
pp. 27-36 ◽  
Author(s):  
Irina Stepanenko ◽  
Semen Yamashkin ◽  
Yuliya Kostina ◽  
Alyona Batarsheva ◽  
Mikhail Mironov
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Biologically Active ◽  
Diffusion Method ◽  
Significant Activity ◽  
Clinical Strains ◽  
Causative Agents ◽  
New Compounds

Introduction. The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. Microorganisms possess an evolutionary adaptive capacity. Non-adherence to the basic principles of rational antibiotic therapy leads to menacing consequences. More and more pathogenic microbes are becoming resistant to two or more antibiotics. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods. Eighteen test-strains of microorganisms and more than 2000 clinical strains of microorganisms, representating the families Micrococcaceae, Streptococcaceae, Enterobacteriaceae, Moraxellaceae, Pseudomonadaceae, Sphingomonadaceae, Xanthomonadaceae were studied for sensitivity to the compounds derived from 4-, 5-, 6- and 7-aminoindoles. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study, as well as a disc diffusion method. Results and discussion. Sensitivity of the test-strains and of clinical strains of microorganisms to the resulting compounds was studied. The compounds based on substituted 4-, 5-, 6-, 7-aminoindoles showed different activity against the test strains and experimental strains of microorganisms in vitro. It was found that the marked antibacterial activity was exhibited by the compounds containing a trifluoromethyl group. The most significant activity was noted in amides and pyrroloquinolones based on 4-aminoindole, 6-aminoindole and 7-aminoindole.The most effective compounds with laboratory codes 5D, 7D, 39D, S3, HD, 4D showed a pronounced antibacterial activity. Conclusion. Antimicrobial activity of the substituted amides and pyrroloquinolines on the basis of 4-, 5-, 6-, 7-aminoindoles was etermined in our study, as well as the spectra of their action against Gram-positive and Gram-negative microorganisms, which are causative agents of non-specific and certain specific human infectious diseases. Moreover, we evaluated the synthetic potentials of the substituted 4-, 5-, 6-, 7-aminoindoles as the starting compounds for synthesizing a series of indolylamides and pyrroloquinolines. Also, the prospects for targeted synthesis of biologically active compounds based on indole-type aromatic amines were determined.

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