PTSA-Catalyzed One Pot Domino Synthesis of Dihydropyrido[2,3-d]pyrimidine Derivatives and their Antimicrobial Activity

2021 ◽  
Vol 6 (3) ◽  
pp. 222-227
Author(s):  
Krishna A. Bhensdadia ◽  
Prakash L. Kalavadiya ◽  
Nilam H. Lalavani ◽  
Shipra H. Baluja
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Pyrimidine Derivatives ◽  
One Pot ◽  
In Vitro Antimicrobial Activity ◽  
Aryl Aldehydes ◽  
Three Component Reaction ◽  
The One

A novel series of dihydropyrido[2,3-d]pyrimidine derivatives were synthesized by multicomponent domino cyclization via the one-pot three component reaction of 6-amino uracil, substituted aryl aldehydes and N-methyl-1-(methylthio)-2-nitroethenamine in the presence of PTSA 10 mol% as a catalyst. The structures of these synthesized compounds were characterized by spectral analysis. Further the synthesized compounds screened for in vitro antimicrobial activity. Among all the compounds, compound 4b containing flouro substitution exhibited good inhibition against the tested species.

scholarly journals Microwave Assisted One Pot Synthesis of Tetrazole Based 3-hydroxy-4H-chromen-4-ones by modified Algar-Flynn-Oyamada reaction and their Antimicrobial activity

2019 ◽  
Vol 63 (4) ◽  
Author(s):  
ASHOK DONGAMANTI ◽  
Nagaraju Nalaparaju ◽  
Sarasija Madderla ◽  
Vijaya Lakshmi Bommidi
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Klebsiella Pneumonia ◽  
Good Activity ◽  
One Pot ◽  
Microwave Assisted ◽  
One Pot Synthesis ◽  
Antimicrobial Studies ◽  
The One

In the present work, we report the one pot synthesis of tetrazole based 3-hydroxy-4H-chromen-4-ones 3(a-g) from  4-(1H-tetrazol-5-yl)benzaldehyde and 2-hydroxy acetophenone using KOH and H2O2 by modified Algar-Flynn-Oyamada reaction under conventional and microwave irradiation conditions. In this technique, flavonols are synthesized without isolating chalcones, in good yields. All the synthesized compounds were characterized by IR, NMR, MS and elemental. All newly synthesized compounds were screened for their in-vitro antimicrobial activity against strains such as Staphylococcus aurous, Bacillus subtilis, Klebsiella pneumonia, Escherichia coli, Aspergillus Niger, Aspergillus flavus, and Fusarium oxysporum. The results of antimicrobial studies revealed that most of the compounds exhibit good activity.

Synthesis, Characterization and Antimicrobial Evaluation of Novel Dimethyl Triazene Incorporated Phenylamino Pyrimidine Derivatives

2021 ◽  
Vol 6 (3) ◽  
pp. 211-216
Author(s):  
Vidhya V. Jadvani ◽  
Yogesh T. Naliapara
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
13C Nmr ◽  
Pyrimidine Derivatives ◽  
In Vitro Antimicrobial Activity ◽  
Fungal Strains ◽  
Elemental Analyses ◽  
Antimicrobial Evaluation ◽  
Hydro Chloride

A series of novel (E)-4-(4-(3,3-dimethyltriaz-1-en-1-yl)phenyl)-N-phenylpyrimidin-2-amine derivatives have been synthesized from the condensation of (E)-3-(dimethylamino)-1-(4-(E)-3,3-dimethyltriaz- 1-en-1-yl)phenyl)prop-2-en-1-one with several guanidinium hydro-chloride. The newly synthesized compounds were examined for in vitro antimicrobial activity against some antibacterial and fungal strains. The synthesized compounds were characterized by 1H NMR, 13C NMR, IR, mass and elemental analyses.

One-Pot Three-Component Synthesis and Molecular Docking of Some Novel 2-Thiazolyl Pyridines as Potent Antimicrobial Agents

2019 ◽  
Vol 19 (6) ◽  
pp. 527-538 ◽  
Author(s):  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Mohamed E.B. Shaaban ◽  
Kamal A. Rabee ◽  
Heba N. El-Shemy ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Antimicrobial Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Binding Affinities ◽  
Thiazole Derivatives ◽  
One Pot ◽  
Three Component Reaction

Background: Thiazoles and pyridines are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential antimicrobial activity. Objective: In the efforts to develop suitable antimicrobia drugs, medicinal chemists have focused on thiazole derivatives. A novel series of 2-thiazolyl pyridines was prepared in a one-pot three-component reaction using 2-bromoacetyl pyridine as a starting precursor. Method: Structure of the synthesized compounds was elucidated by spectral data (FT-IR, 1H NMR, 13C NMR, and mass) and elemental analyses. The prepared compounds were screened for their in vitro antimicrobial activity. Results: The results revealed that compounds 4a,b,e-g and 12 showed promising activity. Molecular docking studies using MOE software were carried out for compounds 4a and 4b which exhibited potent activities indicated by the diameter zones (4a; 3.6, 4.0, 1.2 mm) (4b; 4.2, 3.5, 1.5 mm) and the binding affinities (4a; -5.7731, -5.3576, -4.6844 kcal mol-1) (4b; -5.9356, -2.8250, -5.3628 kcal mol-1) against Candida albicans, Bacillus subtilis and Escherichia coli, respectively. Conclusion: This paper describes a facile and efficient MCR for synthesis of 2-thiazolyl pyridines from reaction of 2-bromoacetyl pyridine with different reagents. There was an agreement between the values of binding affinities and interactions and the data obtained from the practical antimicrobial screening of the tested compounds.

scholarly journals Microwave assisted Synthesis and Antimicrobial Activity of Substituted Pyrrolidinone derivatives

2020 ◽  
Vol 13 (1) ◽  
pp. 227-231
Author(s):  
Marapala Kumara Swamy ◽  
N. Venkatesh ◽  
M. Swapna ◽  
P. Venkateswar Rao
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Aldehydes ◽  
Microwave Assisted Synthesis ◽  
Water Medium ◽  
One Pot ◽  
Standard Drug ◽  
Microwave Assisted ◽  
Three Component Reaction ◽  
Fungal Organisms

A microwave assisted green synthetic methodoloy was developed for the synthesis various substituted pyrrolidinones derivatives by the one-pot three component reaction of aromatic aldehydes, aniline with dialkylbut-2-ynedioate in the presence of p-TsOH in water medium. The compounds were screened for their in vitro antimicrobial activity against four bacterial organism and two fungal organisms, resulted moderate to good activity with compared to their standard drug.

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