scholarly journals Synthesis, Characterization and Biological Evaluation of Novel Tetrasubsituted Imidazole Compounds

2020 ◽  
Author(s):  
khurram shahzad ◽  
Faheem Abbas ◽  
DIGVIJAY PANDEY ◽  
Sanila Ajmal ◽  
Mudassar Khadim ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Primary Amines ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Conductivity Method ◽  
One Pot ◽  
New Class ◽  
Ft Ir ◽  
Uv Visible ◽  
Imidazole Compounds

A new class of tetrasubsituted imidazole based compounds were synthesized using multicomponent one pot synthesis scheme through cyclocondensation reaction of benzil, aromatic primary amines, aldehydes and ammonium acetate in glacial acetic acid. The synthesized compounds have been analyzed and characterized by melting point, color, conductivity method, CHN analysis, FT-IR and UV-Visible. The reaction proceeding was examined by TLC after regular intervals of period. To test biological activity, the synthesized compounds have been examined against various bacterial strains. From the analysis of the antibacterial activity of these synthesized compounds demonstrated that all three imidazole compounds have considerable to significant activity against the strains, and compound K2 was found potent comparatively.<br>

scholarly journals Synthesis, Characterization and Biological Evaluation of Novel Tetrasubsituted Imidazole Compounds

2020 ◽  
Author(s):  
khurram shahzad ◽  
Faheem Abbas ◽  
DIGVIJAY PANDEY ◽  
Sanila Ajmal ◽  
Mudassar Khadim ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Primary Amines ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Conductivity Method ◽  
One Pot ◽  
New Class ◽  
Ft Ir ◽  
Uv Visible ◽  
Imidazole Compounds

A new class of tetrasubsituted imidazole based compounds were synthesized using multicomponent one pot synthesis scheme through cyclocondensation reaction of benzil, aromatic primary amines, aldehydes and ammonium acetate in glacial acetic acid. The synthesized compounds have been analyzed and characterized by melting point, color, conductivity method, CHN analysis, FT-IR and UV-Visible. The reaction proceeding was examined by TLC after regular intervals of period. To test biological activity, the synthesized compounds have been examined against various bacterial strains. From the analysis of the antibacterial activity of these synthesized compounds demonstrated that all three imidazole compounds have considerable to significant activity against the strains, and compound K2 was found potent comparatively.<br>

scholarly journals Synthesis, Characterization and Biological Evaluation of Novel Tetrasubsituted Imidazole Compounds

2020 ◽  
Author(s):  
Khurram Shahzad ◽  
Faheem Abbas ◽  
DIGVIJAY PANDEY ◽  
Sanila Ajmal ◽  
Mudassar Khadim ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Biological Evaluation ◽  
Primary Amines ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Conductivity Method ◽  
One Pot ◽  
New Class ◽  
Ft Ir ◽  
Imidazole Compounds

A new class of tetrasubstituted imidazole based compounds was synthesized using a multicomponent one-pot synthesis scheme through a cyclo condensation reaction of benzil, aromatic primary amines, aldehydes and ammonium acetate in glacial acetic acid. The synthesized compounds have been analyzed and characterized by melting point, color, conductivity method, CHN analysis, FT-IR, and UV-Visible. The reaction proceeding was examined by TLC after regular intervals of period. To test biological activity, the synthesized compounds have been examined against various bacterial strains. From the analysis of the antibacterial activity of these synthesized compounds demonstrated that all three imidazole compounds have considerable to significant activity against the strains, and compound K2 was found potent comparatively.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

scholarly journals A New Supported Manganese-Based Coordination Complex as a Nano-Catalyst for the Synthesis of Indazolophthalazinetriones and Investigation of Its Antibacterial Activity

Chemistry ◽  
2021 ◽  
Vol 3 (3) ◽  
pp. 783-799
Author(s):  
Maryam Ariannezhad ◽  
Davood Habibi ◽  
Somayyeh Heydari ◽  
Vahideh Khorramabadi
Keyword(s):  
Antibacterial Activity ◽  
Simple Procedure ◽  
Condensation Reaction ◽  
Antibacterial Properties ◽  
Coordination Complex ◽  
Bacterial Strains ◽  
One Pot ◽  
Nano Catalyst ◽  
Ft Ir ◽  
The One

A new magnetic supported manganese-based coordination complex (Fe3O4@SiO2@CPTMS@MBOL@ Mn) was prepared in consecutive stages and characterized via various techniques (VSM, SEM, TEM, XRD, FT-IR, EDX, TG-DTA, and ICP). To evaluate its application, it was used for synthesis of divers Indazolophthalazinetriones in a simple procedure via the one-pot three-component condensation reaction of aldehydes, dimedone, and phthalhydrazide in ethanol under reflux conditions. The Mn catalyst can be recycled without any noticeable loss in catalytic activity. Additionally, the antibacterial properties of the nano-catalyst were studied against some bacterial strains.

scholarly journals Synthesis and biological evaluation of triphenyl-imidazoles as a new class of antimicrobial agents

2018 ◽  
Vol 9 (4) ◽  
pp. 369-374 ◽  
Author(s):  
Anupam Anupam ◽  
Mohammed Al-Bratty ◽  
Hassan Ahmad Alhazmi ◽  
Shamim Ahmad ◽  
Supriya Maity ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Dilution Method ◽  
Serum Glutamic Oxaloacetic Transaminase ◽  
Active Compounds ◽  
Lead Compounds ◽  
New Class ◽  
Diffusion Technique ◽  
Ft Ir

Newer triphenyl-imidazole derivatives (4a-h) were synthesized in good yields by the reaction of benzil and substituted benzaldehydes in equimolar quantities and refluxing the product with acetyl chloride thereafter. Structures were confirmed by using FT-IR, 1H NMR and 13C NMR spectroscopic methods. All the synthesized compounds were tested for their antimicrobial activity using agar diffusion technique against Gram positive (Staphhylococcus aureus and Bacillus subtilis), Gram negative (Escherichia coli and Pseudomonas aureginosa) as well as Fungal strain (Candida albicans). Interestingly compounds 4a, 4b, 4f and 4h showed significant antibacterial activity, whereas compound 4b was found to have remarkable activity against the fungal strain. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of most active compounds were determined by broth dilution method and compound 4b emerged to have potent activities against most of the strains having MIC in the range of 25-200 µg/mL. To check the possible toxicities of the most active compounds, they were orally administered in rats and the concentration of liver enzymes serum glutamic-oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase (ALKP) were determined. Compound 4h showed significant increase in the enzymes level depicting the hepatotoxicity. The structure-activity relationship studies showed the importance of electron withdrawing groups at the distant phenyl ring at ortho and para positions as the compounds having chloro or nitro at these positions tend to be more active than the compounds with electron releasing groups such as methoxy. These compounds may act as lead compounds for further studies and appropriate modification in their structure may lead to agents having high efficacy with lesser toxicity.

scholarly journals Promising Antidiabetic and Antimicrobial Agents Based on Fused Pyrimidine Derivatives: Molecular Modeling and Biological Evaluation with Histopathological Effect

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2370
Author(s):  
Fatma Bassyouni ◽  
Mohammad Tarek ◽  
Abeer Salama ◽  
Bassant Ibrahim ◽  
Sawsan Salah El Dine ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
In Vivo Studies ◽  
Total Serum ◽  
Histopathological Study ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Pyrimidine Derivatives ◽  
Reference Drug

Diabetes is the most common metabolic disorder in both developing and non-developing countries, and a well-recognized global health problem. The WHO anticipates an increase in cases from 171 million in 2000 to 366 million by 2030. In the present study, we focus on the preparation of pyrimidine derivatives as potential antidiabetic and antimicrobial agents. Thein vivoeffect on total serum glucose concentration, cholesterol and antioxidant activity was assessed in adult male albino Wister rats and compared to the reference drug glimperide. Promising results were observed for compound 5. The histopathological study confirms that compound 5 results in significant activity with liver maintenance. The antimicrobial activities were evaluated against several bacterial strains such as Salmonella typhimurium ATCC 25566, Bacillus cereus, Escherichia coli NRRN 3008, Pseudomonas aeruginosa ATCC 10145, Staphylococcus aureus ATCC 6538and fungi such as Rhizopus oligosporus, Mucor miehei and Asperillus niger. Compounds 4 and 5 showed a good inhibition of the bacterial zone compared to the reference drug cephradine. Finally, we suggest protein targets for these drugs based on computational analysis, and infer their activities from their predicted modes of binding using molecular modeling. The molecular modeling for compounds 4 and 5 resulted in improved docking scores and hydrogen bonding. The docking studies are in good agreement with the in vitro and in vivo studies.

EXTRACTION, ISOLATION, CHARACTERIZATION, SEMISYNTHESIS AND BIOLOGICAL EVALUATION OF BERBERINE FROM ROOTS OF BERBERIS ARISTATA

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (09) ◽  
pp. 18-24
Author(s):  
J Mittal ◽  
◽  
K. Chaudhary ◽  
N Kumar ◽  
D Pathak
Keyword(s):  
Mass Spectrometry ◽  
Elemental Analysis ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Percolation Method ◽  
Acetophenone Derivatives ◽  
Antibacterial And Antifungal

A methanolic extract of roots of Berberis aristata was prepared by using hot percolation method. Berberine was isolated from the above extract and characterized by IR, 1HNMR, mass spectrometry and elemental analysis. A series of 8-(substituted acetophenone) berberine derivatives was synthesized by introducing various acetophenone derivatives at 8th position of berberine and analyzed by melting point and TLC. The structures of all the synthesized compounds were characterized by IR, 1HNMR, mass spectrometry and elemental analysis. The semisynthesized compounds were screened for in vitro antibacterial and antifungal activity using disc (5mm) diffusion method on nutrient agar medium against Gram-positive (Staphylococcus aureus and Bacillus subtilis), Gram-negative bacterial strains (Pseudomonas aeruginosa and Escherichia coli) and fungal strains (Aspergillus niger and Candida albicans) respectively. The zone of inhibition was compared with standard drugs berberine and kanamycin. All the above compounds showed significant activity in comparison to the standards berberine and kanamycin.

Synthesis, Characterization and Antibacterial Evaluation of 2, 3Dihydroquinazolin-4 (1H)-Ones and Some New Bis 2, 3-Dihydroquinazolin-4 (1H)-Ones Using Pre-made Pyrazole Carbaldehyde Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Kiana Faraji Sina ◽  
Asieh Yahyazadeh ◽  
Nosrat Ollah Mahmoodi
Keyword(s):  
Micrococcus Luteus ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
One Pot ◽  
Montmorillonite K10 ◽  
Recoverable Catalyst ◽  
Ft Ir ◽  
High Yields ◽  
Short Times

: 2, 3-Dihydroquinazolinones are of popular compounds with the diversification of biological and pharmacological activities. Among many discovered methods, there are efficient and convenient methods used for the synthesis of 2, 3- dihydroquinazoline-4 (1H)-one and some new bis 2, 3-dihydroquinazoline-4 (1H)-one derivatives which are reported in this study. The mentioned methods include the two-component condensation of one molecule of anthranilamide and one molecule of DOI: pyrazole carbaldehyde using montmorillonite-K10 as a catalyst for the preparation of 2, 3 dihydroquinazoline4 (1H)-ones. Also, one-pot pseudo-five-component reaction (5MCRs) of two molecules of isatoic anhydride, two molecules of pyrazole carbaldehydes and one molecule of ethan-1, 2-diamine in the presence of the recoverable catalyst (montmorillonite-K10) for the synthesis of bis 2, 3-dihydroquinazoline-4 (1H)-ones. Despite the short times of reactions, high yields of products were obtained, which were validated using FT-IR, 1HNMR, 13CNMR, and elemental analysis. Moreover, the compounds were screened for their antimicrobial activities against two-gram-positive bacterial strains: Staphylococcus aureus and Micrococcus Luteus; and against two-gram-negative bacterial strains, as well: Escherichia coli and Pseudomonas aeruginosa, which all were utilized for antibacterial investigations. The results showed moderate or significant antibacterial activities.

Synthesis and Biological Evaluation of a New Schiff Base and its Cu(II) Complex

2017 ◽  
Vol 68 (3) ◽  
pp. 586-588
Author(s):  
Gladiola Tantaru ◽  
Antonia Poiata ◽  
Nela Bibire ◽  
Alina Diana Panainte ◽  
Mihai Apostu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Elemental Analysis ◽  
Schiff Base Ligand ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

A new Schiff base ligand, N-hydroxy-N�-salicylidene-urea was synthesized through the condensation of salicylaldehyde with hydroxyurea. The copper(II) complex of the Schiff base has been also obtained. Their structure has been proven using spectral methods such as UV-Vis, FT-IR, 1H-NMR and elemental analysis. The antimicrobial activity of the copper(II) complex was evaluated through comparison to the activity of the Schiff base on various bacterial strains. All tested compounds were very active against both gram-positive and gram-negative bacteria.

scholarly journals Eco-Friendly Synthesis, Characterization and Biological Evaluation of Some Novel Pyrazolines Containing Thiazole Moiety as Potential Anticancer and Antimicrobial Agents

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2970 ◽  
Author(s):  
Mastoura Edrees ◽  
Sraa Melha ◽  
Amirah Saad ◽  
Nabila Kheder ◽  
Sobhi Gomha ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Thiazole Ring ◽  
Bacterial Strains ◽  
One Pot ◽  
Grinding Method ◽  
Test Organisms ◽  
The One

The one-pot synthesis of a series of pyrazoline derivatives containing the bioactive thiazole ring has been performed through a 1,3-dipolar cycloaddition reaction of N-thiocarbamoylpyrazoline and different hydrazonoyl halides or α-haloketones in the presence of DABCO (1,4-diazabicyclo[2.2.2] octane) as an eco-friendly catalyst using the solvent-drop grinding method. The structure of the synthesized compounds was elucidated using elemental and spectroscopic analyses (IR, NMR, and Mass). The activity of these compounds against human hepatocellular carcinoma cell line (HepG2) was tested and the results showed that the pyrazoline 11f, which has a fluorine substituent, is the most active. The antimicrobial activities of the newly synthesized compounds were determined against two fungi and four bacterial strains, and the results indicated that some of the newly synthesized pyrazolines are more potent than the standard drugs against test organisms.

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