scholarly journals Microwave-assisted synthesis of new pyrazole derivatives bearing 1,2,3-triazole scaffold as potential antimicrobial agents

2017 ◽  
Vol 82 (4) ◽  
pp. 357-366 ◽  
Author(s):  
Dongamanti Ashok ◽  
Rangu Kavitha ◽  
Srinivas Gundu ◽  
Rao Hanumantha
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Pyrazole Derivatives ◽  
Inhibitory Effects ◽  
Fungal Strains ◽  
Microwave Assisted ◽  
Cuaac Reaction ◽  
Ft Ir

A new series of (E)-3-(3-(4-substituted phenyl)-1-phenyl-1H-pyrazol- 4-yl)-1-(2-hydroxy-4-((1-aryl-1H-1-2,3-triazol-4-yl)methoxy)phenyl)- prop-2-en-1-one derivatives was synthesized. The synthesis of the title compounds involved the 1,3-dipolar Cu(I)-catalyzed alkyne?azide cycloaddition (CuAAC) reaction of (E)-3-(3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4- -yl)-1-(2-hydroxy-4-(prop-2-yn-1-yloxy)phenyl)prop-2-en-1-ones with aromatic azides. The structures were confirmed by NMR, FT-IR, mass and elemental analysis. All the synthesized compounds (6a?j) were evaluated for their antimicrobial activity. Compounds 6a, 6d and 6e demonstrated promising inhibitory effects on both bacterial and fungal strains.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<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>

scholarly journals Synthesis and Evaluation of Some Novel Chromone Based Dithiazoles as Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naureen Aggarwal ◽  
Vishal Sharma ◽  
Harpreet Kaur ◽  
Mohan Paul Singh Ishar
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Fungal Strains ◽  
Inhibitory Potential ◽  
C Nmr

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

scholarly journals Microwave Assisted Synthesis of some Novel Sulphonamide Bearing Pyrazolone Core Structure

2014 ◽  
Vol 30 ◽  
pp. 116-126
Author(s):  
Dipti L. Namera ◽  
Khushal M. Kapadiya ◽  
Mitesh M. Chhatrola ◽  
Umed C. Bhoya
Keyword(s):  
Experimental Data ◽  
Conventional Method ◽  
Mass Spectroscopy ◽  
Elemental Analysis ◽  
Microwave Assisted Synthesis ◽  
H Nmr ◽  
Microwave Assisted ◽  
Pyrazolone Derivatives ◽  
Ft Ir ◽  
Microwave Assisted Method

We have described some novel Sulphonamide bearing pyrazoline derivatives synthesized by conventional method as well as microwave assisted method of synthesis. The reaction of 4-(3-methyl-5-oxo-4,5-dihydro-1-H-pyrazol-1-yl)benzenesulphonamide with substituted benzaldehyde in the presence of Methanol as solvent and piperidine as catalyst, generated a series of substituted pyrazolone derivatives 4a-m. The structures of all synthesized compounds are well characterized by Mass spectroscopy, FT-IR, 1H NMR and elemental analysis. After obtaining experimental data regarding the yield and the time taken for the synthesis by both the approaches, convenient and microwave assisted method, it was ascertained that the microwave assisted method is more suitable for synthesis of pyrazolone derivatives 4a-m.

Synthesis, photosensitization and antimicrobial activity evaluation of some novel Merocyanine dyes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Aspergillus Flavus ◽  
Elemental Analysis ◽  
Cyanine Dyes ◽  
Fungal Strains ◽  
Activity Evaluation ◽  
Visible Spectra ◽  
Merocyanine Dyes

Novel acyclic and cyclic merocyanine dyes derived from the nucleu of furo [(3,2-d) pyrazole; ( d 2 , 3 )imidazole]were prepared. The electronic visible absorptionspectra of all the synthesized new cyanine dyes were examined in 95% ethanolsolution to evaluate their photosensitization properties. Antibacterial andantifungal activities for some selected dyes were tested against various bacterialand fungal strains (Escherichia coli, Staphylococcus aureus, Aspergillus flavus andCandida albicans) to evaluate their antimicrobial activity. Structural identificationwas carried out via elemental analysis, visible spectra, IR and 1H NMRspectroscopic data.

Microwave assisted synthesis of novel Pyrazole derivatives and their biological evaluation as anti-bacterial agents

2020 ◽  
Vol 23 ◽  
Author(s):  
Hadis Khodadad ◽  
Farhad Hatamjafari ◽  
Khalil Pourshamsian ◽  
Babak Sadeghi
Keyword(s):  
Antibacterial Activity ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Antibacterial Activities ◽  
Structural Features ◽  
Biological Evaluation ◽  
Aureus Strain ◽  
Microwave Assisted Synthesis ◽  
Pyrazole Derivatives ◽  
Microwave Assisted

Aim and Objective: Microwave-assisted condensation of acetophenone 1 and aromatic aldehydes 2 gave chalcone analogs 3, which were cyclized to pyrazole derivatives 6a-f via the reaction with hydrazine hydrate and oxalic acid in the presence of the catalytic amount of acetic acid in ethanol. Materials and Methods: The structural features of the synthesized compounds were characterized by melting point, FT-IR, 1H, 13C NMR and elemental analysis. Results: The antibacterial activities of the synthesized pyrazoles was evaluated against three gram-positive bacteria such as Enterococcus durans, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria such as Escherichia coli and Salmonella typhimurium. Conclusion: All the synthesized pyrazoles showed relatively high antibacterial activity against S. aureus strain and none of them demonstrated antibacterial activity against E. coli.

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Activities of Some 2-Amino-4-aryl-3-cyano-6-(4’-hydroxy phenyl)-pyridines

2011 ◽  
Vol 8 (1) ◽  
pp. 119-122 ◽  
Author(s):  
Priya Gothwal ◽  
Gunwanti Malhotra ◽  
Y. K. Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Ammonium Acetate ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted

4’-Hydroxy chalcones were treated with malononitrile in the presence of ammonium acetate under solventless microwave assisted condition to get 2-amino-4-aryl-3-cyano-6-(4’-hydroxy phenyl)-pyridines. The prepared compounds were screened for their antimicrobial activity; some of them have exhibited promising antimicrobial activity.

Sign in / Sign up

Export Citation Format

Share Document