scholarly journals Bicyclic [1,3,4]Thiadiazolo[3,2-α]Pyrimidine Analogues: Novel One-Pot Three-Component Synthesis, Antimicrobial, and Antioxidant Evaluation

2021 ◽  
Vol 11 (5) ◽  
pp. 12925-12936
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Sulfonic Acid ◽  
Aromatic Aldehydes ◽  
One Pot ◽  
Antibacterial And Antifungal Activities ◽  
Toluene Sulfonic Acid ◽  
Antioxidant Evaluation ◽  
Pyrimidine Analogues ◽  
Antibacterial And Antifungal

A novel one-pot three-component synthesis of 1-(7-methyl-2,5-diphenyl-5H-[1,3,4]thiadiazolo(3,2-α)pyrimidine-6-yl)ethanone (4a-i) derivatives via cyclo-condensation of substituted 2-amino-[1,3,4]thiadiazole (1a-c), acetylacetone (2) and various aromatic aldehydes (3a-c) in the presence of p-toluene sulfonic acid (PTSA) in acetonitrile. Spectral data and elemental analysis have characterized the newly synthesized compounds. The new analogs were screened for their antibacterial and antifungal activities. The majority of the tested compounds displayed significant to moderate efficacy against most of the designated organisms. Among the tested compounds, 4b, 4e, and 4h showed noteworthy efficacy against selected microbes, and compounds 4c and 4i were found to be exceptionally efficient against selected fungal strains. Compound 4c, 4e, 4f, 4i were also designated as best antioxidants against NOx.

scholarly journals Synthesis of selected 5-thio-substituted tetrazole derivatives and evaluation of their antibacterial and antifungal activities

2011 ◽  
Vol 76 (2) ◽  
pp. 165-175 ◽  
Author(s):  
V. Dhayanithi ◽  
Syed Shafi ◽  
K. Kumaran ◽  
Sankar Jai ◽  
Venkat Ragavan ◽  
...  
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Sodium Azide ◽  
Second Step ◽  
Benzyl Isothiocyanate ◽  
Step Process ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Tetrazole Derivatives

Several 5-thio-substituted tetrazole derivatives were efficiently synthesized by a three-step process. The substituted tetrazol-5-thiol, namely, 1-benzyl-1H-tetrazol-5-thiol (2) was prepared by refluxing commercially available benzyl isothiocyanate (1) with sodium azide in water. The second step was the synthesis of 1-benzyl-5-[(3-bromopropyl) thio]tetrazole (3) by thio alkylation of tetrazol-5-thiol (2) with 1,3- dibromopropane in tetrahydrofuran. Finally, the 5-thio-substituted tetrazole derivatives 4a-i were prepared by condensation of (3) with the corresponding amine or thiol. The structures of the newly synthesized compounds were characterized by NMR, LC/MS/MS, IR spectral data and elemental analysis. All the synthesized compounds were screened for their antibacterial and antifungal activities.

scholarly journals Thiazolo-Pyrimidine Analogues: Synthesis, Characterization and Docking Studies Guided Antimicrobial Activities

2020 ◽  
Vol 11 (2) ◽  
pp. 9443-9455
Keyword(s):  
Aromatic Aldehydes ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
One Pot ◽  
Standard Drug ◽  
Toluene Sulfonic Acid ◽  
Pyrimidine Analogues

In the current study, bicyclic 1-(7-methyl-3,5-diphenyl-5H-thiazolo(3,2-α)pyrimidine-6-yl)ethanone (4a-l) derivatives have been designed and conveniently synthesized by one-pot three-component method via cyclocondensation of substituted 4-phenylthiazole-2-amine (1a-c), acetylacetone (2) and various aromatic aldehydes (3a-d) in the presence of p-toluene sulfonic acid (PTSA) under acetonitrile solvent medium. The synthesized compounds (4a-l) have been characterized by spectral analysis and subjected to docking study against protein DNA gyrase (PDB Code: 1KZN), and also, the compounds were screened for their in vitro antimicrobial activities. The bioassay of the synthesized compounds envisioned that the compound 4k emerged as a broad-spectrum antibacterial agent, and 4l emerged as a good antifungal agent compared to standard drug.

scholarly journals Synthesis and Biological Activity of (Z) –n-(5-Benzylidene-4-oxo-2-substituted- phenylthiazolidin-3-yl)-5-((1, 3-dioxoisoindolin-2-yl)methyl)-2-hydroxybenzamide

2010 ◽  
Vol 7 (4) ◽  
pp. 1484-1490
Author(s):  
M. C. Patel ◽  
Dhameliya
Keyword(s):  
Biological Activity ◽  
Spectral Data ◽  
Thioglycolic Acid ◽  
Aromatic Aldehydes ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

5-((1, 3-Dioxoisoindolin-2-yl)methyl-2-hydroxybenzohydrazide (1) undergoes facile condensation with aromatic aldehydes to afford the correspondingN'-substituted-phenyl-5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxybenzohydrazide (2a-h) in good yields. Cyclocondensation of compounds (2a-h) with thioglycolic acid yields 5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxy-N-(4-oxo-2-substituted phenylthiazolidin-3-yl)benzamide (3a-h). These (3a-h) compounds were further reacted with benzaldehyde in the presence of sodium ethanolate affords, (Z) –N-(5-benzylidene-4-oxo-2-substituted phenyl-thiazolidin-3-yl)-5-((1,3-dioxoisoindolin-2-yl)methyl)-2-hydroxybenzamdie(4a-h). The structures of these compounds were established on the basis of analytical and spectral data. All the newly synthesized compounds were evaluated for their antibacterial and antifungal activities.

scholarly journals Synthesis and Antimicrobial Activity of Some Novel Substituted Piperazinyl-quinazolin-3(4H)-ones

2008 ◽  
Vol 5 (1) ◽  
pp. 23-33 ◽  
Author(s):  
N. M. Raghavendra ◽  
P. P. Thampi ◽  
P. M. Gurubasavarajaswamy
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Single Step ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Single Step Reaction

Several substituted-quinazolin-3(4H)-ones were synthesized by condensation of 2-chloro-N-(4-oxo-substituted-quinazolin-3(4H)-yl)-acetamides with various substituted piperazines through single step reaction. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antibacterial and antifungal activities.

Design, Synthesis, Antimicrobial Evaluation and Molecular Modeling Study of New 2-mercaptoimidazoles (Series-III)

2019 ◽  
Vol 16 (5) ◽  
pp. 512-521 ◽  
Author(s):  
Nidhi Rani ◽  
Randhir Singh
Keyword(s):  
Sulfonic Acid ◽  
Docking Study ◽  
Molecular Docking Study ◽  
One Pot ◽  
Design Synthesis ◽  
Toluene Sulfonic Acid ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi ◽  
High Yields ◽  
Antimicrobial Potency

Background: A series of novel substituted 2-mercaptoimidazoles was synthesised efficiently and in high yields using one-pot synthesis from m-hydroxyacetophenones. Methods: The structures of the newly synthesized compounds were established, their molecular activity was investigated against some bacteria and fungi were further validated using molecular docking study. Results: Reaction of o-hydroxyphenacylbromide (2) with substituted aniline and KSCN, in the presence of catalyst p-toluene sulfonic acid afforded 4(a-r) in good yield. The structure of compounds (4a-r) was confirmed by IR, NMR and MS. Conclusion: The compounds exhibited excellent antimicrobial potency against the tested microorganism.

scholarly journals Synthesis and antimicrobial activities of some (E)-N'-1-(substituted benzylidene)benzohydrazides

2017 ◽  
Vol 5 (1) ◽  
pp. 17 ◽  
Author(s):  
V. Manikandan ◽  
S. Balaji ◽  
R. Senbagam ◽  
R. Vijayakumar ◽  
M. Rajarajan ◽  
...  
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Fourier Transform ◽  
Magnetic Resonance ◽  
Spectral Data ◽  
Ultra Violet ◽  
Antimicrobial Activities ◽  
Antibacterial And Antifungal Activities ◽  
Ft Ir ◽  
Fourier Transform Ir ◽  
Antibacterial And Antifungal

About ten substituted (E)-N'-1-(substituted benzylidene) benzohydrazides have been synthesized. They are analyzed by their analytical, ultra violet (UV), Fourier transform-IR (FT-IR) and nuclear magnetic resonance (NMR) spectral data and evaluated by antimicrobial activities such antibacterial and antifungal activities.

Synthesis and Characterization of Substituted μ-oxo-bis[tetra-phenylporphyrinatoiron] Compounds

2015 ◽  
Vol 748 ◽  
pp. 183-186
Author(s):  
Zhi Cheng Sun ◽  
Shu Ying Chen ◽  
Zhi Peng Guo ◽  
Mei Juan Cao ◽  
Lu Hai Li
Keyword(s):  
Infrared Spectra ◽  
Elemental Analysis ◽  
Aromatic Aldehydes ◽  
Synthesis And Characterization ◽  
Visible Spectroscopy ◽  
Reaction Conditions ◽  
One Pot ◽  
Optimum Reaction ◽  
Novel Method

A novel one-pot method for the synthesis of substituted μ-oxo-bis [tetraphenyl porphyrinatoiron] compounds ([TRPPFe]2O) from pyrrole and aromatic aldehydes was proposed and investigated in this paper. Four kinds of [TRPPFe]2O were designed and synthesized by one-pot reaction and characterized by elemental analysis, infrared spectra and ultraviolet-visible spectroscopy. Moreover, the [TRPPFe]2O yields of 18.7~22.4% could be obtained with this novel method under the optimum reaction conditions.

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