Synthesis and Antimicrobial Evaluation of Quinazoline-4[3H]-one Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Cheenu Chaudhary ◽  
Sushil Kumar ◽  
Surendra Kumar ◽  
S. Riaz Hashim
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Spectroscopic Method ◽  
Catalytic Amount ◽  
Binding Affinities ◽  
Zone Of Inhibition ◽  
Plate Method ◽  
Standard Drug ◽  
Antimicrobial Evaluation

: The present investigation aim to synthesize quinazoline-4(3H)-one derivatives (B1-10) and evaluation for their antimicrobial activity. The test compounds (B1-10) were obtained by reaction of 2-phenyl-4H-benzo[d] [1, 3]oxazin-4-one (1) with 4-aminophenol (2) to afford 3-(4-hydroxyphenyl)-2-phenylquinazoline-4(3H)-one (3) which further reacted with different N-phenylacetamide (4) in presence of anhydrous potassium carbonate and catalytic amount of potassium iodide in ethylmethylketone. The test compounds (B1-10) were characterized by spectroscopic method and evaluated for their antimicrobial activity using cup plate method by measuring zone of inhibition. Among the compounds, compound B1, B2, B4, B6 and B8 showed maximum zone of inhibition as compare with standard drug ciprofloxacin and fluconazole against Bacillus subtilis, Escherichia coli and Aspergillus niger. Molecular docking was also performed for test compounds to predict their binding affinities in the target protein and results showed good drug-like properties

scholarly journals Synthesis, Characterization and Antimicrobial Evaluation of some 1,2,4-Triazolo-5-Thione Derivatives

2021 ◽  
Vol 11 (1) ◽  
pp. 24-30
Author(s):  
Gurdeep Singh ◽  
◽  
Neetesh K. Jain ◽  
Kiran Sahu ◽  
◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Melting Point ◽  
Agar Plate ◽  
Aromatic Aldehydes ◽  
Plate Method ◽  
Antimicrobial Drugs ◽  
Standard Drug ◽  
New Antibiotics ◽  
Antimicrobial Evaluation

Due to this increasing predicament of antibiotic confrontation, the lot of distinct antibiotics available is dwindling and there are only smatterings of new antibiotics in the drug development channel. Therefore, an intense necessitate for new antimicrobial drugs. In current study, substituted 1,2,4-triazolo-5-thione derivatives were synthesized from substituted aromatic aldehydes, succinic acids and the structure of synthesized compounds were established by physicochemical (Melting Point, Rf value) and spectral analysis (IR, NMR & Mass). The title compounds were then evaluated for their antimicrobial activity against ciprofloxacin as a standard drug using agar plate method. Among all synthesized derivatives A5 and A6 found were found to possess very promising antimicrobial activity. Keywords: 1,2,4-triazolo-5-thione, anti-microbial, antibiotic, thione, Ciprofloxacin.

scholarly journals Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Property ◽  
Docking Study ◽  
Gram Negative Bacteria ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Comparable Activity ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

scholarly journals Synthesis of Novel Diclofenac Hydrazones: Molecular Docking, Anti-Inflammatory, Analgesic, and Ulcerogenic Activity

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Nawaf A. Alsaif ◽  
Mashooq A. Bhat ◽  
Mohamed A. Al-Omar ◽  
Hanaa M. Al-Tuwajiri ◽  
Ahmed M. Naglah ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Analgesic Activity ◽  
Binding Affinities ◽  
Standard Drug ◽  
Reference Drug ◽  
Ulcerogenic Activity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Sparing Effect ◽  
Cox 1

This study was aimed to design novel diclofenac hydrazones having anti-inflammatory and analgesic activity with gastric sparing effect. A new series of 2-[2-(2,6-dichloroanilino)phenyl]-N’-[(substituted phenyl) methylidene] acetohydrazide derivatives (1−14) were synthesized and evaluated for their anti-inflammatory, analgesic, and ulcerogenic activity. The compounds were identified and confirmed by elemental analysis and spectral data. During anti-inflammatory activity by carrageenan-induced paw edema method, compounds (2, 3, 7, 8, 11, and 13) were found to be most promising. Compounds 3, 8, and 13 have been found to have significant analgesic activity compared to the reference drug diclofenac in analgesic activity by both the hot plate method and acetic acid-induced writhing method. The compounds which presented highly significant anti-inflammatory and analgesic activity were further tested for their ulcerogenic activity. Compounds 3 and 8 showed maximum ulcerogenic reduction activities. Compound 8 was found to have LD50 of 168 mg/kg. Compound 8 with 3,5-dimethoxy-4-hydroxyphenyl substitution was found to be the most promising anti-inflammatory and analgesic agent with gastric sparing activity. Molecular docking of compounds was performed for COX−1/COX−2 binding site. Lead compound 8 showed better binding affinities of −9.4 kJ/mol with both COX-1 and COX-2 as compared to the standard drug, diclofenac with binding affinities of −6.6 kJ/mol and −8.1 kJ/mol for COX−1 and COX−2, respectively.

scholarly journals STUDY OF ANTIMICROBIAL ACTIVITY OF SILVER-DOPED HYDROXYAPATITE

2019 ◽  
pp. 243-245
Author(s):  
HIBU WAHID ◽  
ANJUVAN SINGH
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Fourier Transform ◽  
Infrared Spectroscopy ◽  
Fourier Transform Infrared Spectroscopy ◽  
Xrd Analysis ◽  
Chemical Precipitation ◽  
Silver Concentration ◽  
Precipitation Method ◽  
Zone Of Inhibition

Objective: Hydroxyapatite (Hap) is an important material used for implants because of its structural similarity with calcium phosphate of the teeth and bones. Hap is mostly used in the situations where load-bearing implants are needed, such as in dental and orthopedic applications. Dental plaque is caused due to the bacteria which induces secondary caries through microleakage between the restoration and the tooth structure. Methods: An attempt has been made to provide materials with antibacterial activity by incorporating an antibacterial agent into the chemical mixture (Hap). This study delineates the process of synthesizing silver-doped Hap (Ca10Agx(PO4)6(OH)2) by wet chemical precipitation method and by varying the silver concentration (0.3%–0.5%). The synthesized silver-doped Hap was further characterized using Fourier transform infrared spectroscopy and X-ray diffraction (XRD) analysis. The antimicrobial activities were tested against Gram-negative bacteria Escherichia coli. Results: The maximum zone of inhibition against Escherichia coli was observed when equal concentration of Hydroxyapatite and Silver were mixed together i.e XAg=0.5% Zone of inhibition helps to determine the antimicrobial activity of silver-doped Hap. An increase in the zone of inhibition indicates the least growth of microorganisms which was observed at a silver concentration XAg=0.5%. Conclusions: Silver-doped Hap was synthesized successfully using the chemical precipitation method and was characterized using Fourier transform infrared spectroscopy and XRD analysis. It can be concluded that silver-doped Hap can be an excellent substitute material used as dental implant device.

scholarly journals Assessment of antimicrobial activity of Cola milleni seed and pulp extracts against Staphylococcus aureus, Escherichia coli and Penicillium notatum

2020 ◽  
Vol 12 (1) ◽  
pp. 71-75
Author(s):  
A.M. Aliyu ◽  
S.J. Oluwafemi ◽  
S. Kasim
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Ethanol Extract ◽  
Bioactive Components ◽  
Zone Of Inhibition ◽  
Penicillium Notatum ◽  
Standard Techniques

All over the world, hundreds of plants have been identified based on researchers and experimental evidence as good sources of medicinal agents. The bioactive components (phytochemicals) of both the seeds and pulp of Cola milleni were extracted using ethanol as solvent. The bioactive components detected were alkaloids, tanins, saponins, cardiac glycosides, carbohydrates, sterols, resins and terpenes while Flavonoids, anthraquinones, anthracyanides and phenol were not detected for both the seed and pulps. Antimicrobial activity of the ethanol extract (Seed and pulp) against Staphylococcus aureus, Escherichia coli and Penicillium notatum was carried out using standard techniques. Staphylococcus aureus had the highest zone of inhibition for pulp having a range of 9.7mm±0.58mm - 19.7mm±2.52mm while Penicllium notatum had the least with 0.00mm. S.aureus also had the highest zone of inhibition range of 14.3mm±2.08mm - 21.3mm±1.53mm for the seed extract while penicillium had the least inhibition range of 5.0mm±1.00mm - 5.7mm±0.58. E.coli showed the highest minimum inhibitory concentration with ethanol extract of the pulp (160mg/ml) while penicillium notatum was not reactive. The minimum inhibitory concentration of seed against penillium notatum was the highest (160mg/ml) while staphylococcus aureus showed the lowest of 40mg/ml. The antimicrobial activity is as a result of the presence of phytochemicals detected, which suggest the use of the plant for the treatment of diseases caused by these organisms. Key words: Cola millenii, Phytochemical, Antimicrobial activity, Bacteria, Fungi

scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Positive Control ◽  
Design Synthesis ◽  
Aspergillus Brasiliensis ◽  
In Vitro Investigation ◽  
Bacillus Subtilis Atcc ◽  
Antimicrobial Evaluation

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

scholarly journals Antimicrobial Activity of Crinum defixum Ker - Gawler Leaves

2015 ◽  
Vol 46 ◽  
pp. 8-15
Author(s):  
A. Elaiyaraja ◽  
G. Chandramohan ◽  
J. Mariajancyrani
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Leaf Extract ◽  
Phytochemical Screening ◽  
Zone Of Inhibition ◽  
Indigenous Medicine ◽  
Leaf Extracts ◽  
Mean Diameter ◽  
Different Types ◽  
Body Ache

Crinum defixum Ker - Gawler is a bulbous herb which has widely used in indigenous medicine for many diseases; mainly leaf and bulb extracts are of medicinal importance. Leaf extract is used as a treatment for pimples, body-ache, dropsy, carbuncle, paronychia, leprosy, fever and diarrhoea. The bulbs are crushed and applied on to piles and itching. The present study to determine the possible phytochemicals and antimicrobial activity of various leaf extracts of Crinum defixum Ker - Gawler plant. The phytochemical screening demonstrated the presence different types compound like flavonoids, tannins, phenolic compounds, saponins and glycosides. The ethanol, methanol and crude extracts of Crinum defixum Ker - Gawler showed significant antibacterial activity against Escherichia coli, Staphylococcus aureus, pseudomonas aeruginosa, proteus vulgaris and antifungal activity against Candida albicans, Aspergillus flavus when compare to different concentrations (μg/mL). The antimicrobial potential of test compounds was determined on the basis of mean diameter of zone of inhibition around the disk in millimetres. Thus, the present findings revealed the medicinal potential of Crinum defixum Ker - Gawler to develop a drug against various human ailments.

scholarly journals Antimicrobial, Phytochemical Analysis and Molecular Docking (In-silico Approach) of Tithonia diversifolia (Hemsl.) A. Gray and Jatropha gossypiifolia L on Selected Clinical and Multi-Drug Resistant Isolates

2020 ◽  
pp. 1-18
Author(s):  
A. F. Okiti ◽  
O. T. Osuntokun
Keyword(s):  
Escherichia Coli ◽  
Molecular Docking ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Phytochemical Analysis ◽  
Drug Resistant ◽  
Tithonia Diversifolia ◽  
Zone Of Inhibition ◽  
Zones Of Inhibition ◽  
Jatropha Gossypiifolia

The aim of this study is to determine the zones of inhibition, phytochemical screening and molecular docking (In-silico Approach) of Tithonia diversifolia (Hemsl.) A. Gray and Jatropha gossypiifolia L against selected clinical and multi drug resistant isolates. Crude extraction of air dried leaves were carried out by soaking the plant in ethanol and ethyl acetate, standard agar diffusion method was used for sensitivity testing, minimum inhibitory concentration and minimum bactericidal concentration values were obtained by agar dilution method. The antimicrobial activity of the leaf extracts of T. diversifolia (Hemsl.) A. Gray and J. gossypiifolia L was assayed against Bacillus subtilis, Escherichia coli, Klebsiella pneumonia, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella typhi, Shigella dysentriae, Staphylococcus aureus, Streptococcus pyogenes, Candida albican and against multi drug resistant bacteria which are Acinetobacter baumannii, Enterobacter agglomerans, Proteus mirabilis, Providencia stuartii, Salmonella subsp 3b. Levofloxacin and fluconazole were the standard antibiotics used. Sensitivity test revealed the highest zone of inhibition observed for J. gossypiifolia L and T. diversifolia (Hemsl.) A. Gray against Candida albican with mean and standard deviation of 29±1.414 and 19.5±0.707 at 100 mg/ml respectively, while the least zone of inhibition was observed from the extracts of J. gossypiifolia L against Escherichia coli with 11.75±0.354 at 100 mg/ml. Both plant extracts showed antimicrobial activity against multi drug resistant isolates having zones of inhibition ranging from 0 to 15±1.414. The Minimum Inhibitory Concentration of the extracts ranges between 6.25 and 100 mg/ml as well as the Minimum Bactericidal Concentration. The qualitative and quantitative phytochemical analysis showed the presence of alkaloids, anthraquinone, cardiac glycosides, flavonoids, phlobotannins, reducing sugars saponins, steroids and tannins. Molecular docking of the phytochemicals of T. diversifolia (Hemsl.) A. Gray only was carried out using levofloxacin as template, which revealed the presence of compounds more effective in inhibiting DNA gyrase enzyme. Thus, the use of both plants as traditional medicine is justifiable and should be encouraged in the formulation and production of new antibiotics.

scholarly journals Study of Antibacterial Activity of Chenopodium album Leaves Extract

2018 ◽  
Vol 10 (01) ◽  
Author(s):  
Kaur M. ◽  
Sharma S. ◽  
Garg S. ◽  
Arora M.
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Chenopodium Album ◽  
Antibacterial Activities ◽  
Maximum Activity ◽  
Zone Of Inhibition ◽  
Plate Method ◽  
E Coli ◽  
Test Organisms

This study describes the antibacterial activities of three different solvent extracts of leaves of Chenopodium album. Methanol, acetone and chloroform extracts of C. album were prepared. The antibacterial activity was assessed using well plate method and were examined for the size of zone of inhibition. Different extracts were investigated against the test organisms namely Lactobacillus, Bacillus subtilis and Escherichia coli. The maximum activity was observed at 100% concentration of different extracts of leaves. The maximum zone of inhibition for 100% concentration were observed as E. coli (19 mm) and Lactobacillus (19 mm) in diameter respectively. C. album did not show any antibacterial activity against B. subtilis. Antibacterial activity was compared with standard Amoxicillin and it was found to be 23 mm diameter for Lactobacillus and 25 mm for both E. coli and B. subtilis in terms of zone of inhibition.

scholarly journals Synthesis, Molecular Docking and Antimicrobial Activities of 5-(4-substituted-benzyl)-2-(furan/thiophen-2-ylmethylene hydrazono)thiazolidin-4-ones

2021 ◽  
Vol 11 (4) ◽  
pp. 12434-12446
Keyword(s):  
Escherichia Coli ◽  
Molecular Docking ◽  
1H Nmr Spectroscopy ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Binding Affinities ◽  
Bacterial Strains ◽  
Effective Synthesis

In our present work, we reported an effective synthesis, molecular docking, and antimicrobial properties of novel 5-(4-substituted-benzyl)-2-(furan/thiophen-2-ylmethylene hydrazono) thiazolidin-4-ones (6a-g) and (7a-i). The structures of the synthesized compounds (6a-g) and (7a-i) were elucidated by 1H-NMR spectroscopy. The molecular docking studies were performed for all the synthesized compounds against GlcN-6P using AutoDock-tools-1.5.6 and recorded the extent of H-bonding and binding affinities. The preselected compounds via molecular docking were further tested for in vitro antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial findings exhibited that the compounds possessed significant antimicrobial potential.

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