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.

scholarly journals Microwave-assisted synthesis of 2,8-di(alkyl/aryl)-4,6-dichloro-2H,8H-pyrano[3,2-g] chromene-3,7-dicarbaldehydes and their antimicrobial activity

2019 ◽  
Vol 84 (4) ◽  
pp. 355-364
Author(s):  
Rupireddy Venkataramana ◽  
Venkata Chittireddy ◽  
Dongamanti Ashok ◽  
Kudle Rao
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Aromatic Aldehydes ◽  
Conventional Heating ◽  
Microwave Assisted Synthesis ◽  
Good Activity ◽  
One Pot ◽  
Alkyl Aryl ◽  
Microwave Assisted ◽  
Bacteria And Fungi

A series of 2,8-di(alkyl/aryl)-substituted bischromanone derivatives were synthesized in one pot from 4,6-diacetylresorcinol and aliphatic/aromatic aldehydes in the presence of pyrrolidine/piperidine under conventional heating and microwave irradiation. The 2,8-di(alkyl/aryl)-substituted bischromanones were converted into a new series of 4,6-dichloro-3,7-diformyl-2,8-di(alkyl/aryl)-substituted bischromenes using the Vilsmeier?Haack reagent. The structures of the compounds were established based on elemental analysis, IR, 1H-NMR, 13C- -NMR and LC?MS spectral data. All the synthesized compounds were evaluated for their antimicrobial activity. Some of the compounds showed very good activity compared to standard drugs against all the tested pathogenic bacteria and fungi.

Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
High Yield ◽  
Breast Cancer Cell Lines ◽  
Pyridine Derivatives ◽  
One Pot ◽  
Standard Drug ◽  
Three Component Reaction ◽  
Anti Cancer

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

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.

scholarly journals Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives

2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Mass Spectral Data ◽  
Pyrimidine Derivatives ◽  
Plate Method ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
New Compounds

The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidines 1a-j are compared with those of known chosen standard drugs, viz. ampicillin, chloramphenicol, ciprofloxacin, norfloxacin and griseofulvin. .

scholarly journals One-Pot Microwave-Assisted Synthesis of Carbon Dots and in vivo and in vitro Antimicrobial Photodynamic Applications

2021 ◽  
Vol 12 ◽  
Author(s):  
María Paulina Romero ◽  
Fernanda Alves ◽  
Mirian Denise Stringasci ◽  
Hilde Harb Buzzá ◽  
Heloísa Ciol ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Carbon Dots ◽  
Microwave Assisted Synthesis ◽  
One Pot ◽  
Blue Led ◽  
Led Light ◽  
Microwave Assisted

Graphical AbstractBrief description of the procedures carried out in this study. In vivo and in vitro antibacterial photodynamic therapy (aPDT) studies, where aPDT mediated by C-DOTS and blue LED light against S. aureus was evaluated.

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 Design, Microwave-Assisted Synthesis and In Silico Prediction Study of Novel Isoxazole Linked Pyranopyrimidinone Conjugates as New Targets for Searching Potential Anti-SARS-CoV-2 Agents

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6103
Author(s):  
Faisal K. Algethami ◽  
Maher Cherif ◽  
Salma Jlizi ◽  
Naoufel Ben Ben Hamadi ◽  
Anis Romdhane ◽  
...  
Keyword(s):  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
Microwave Assisted Synthesis ◽  
Dimroth Rearrangement ◽  
One Pot ◽  
Microwave Assisted ◽  
Three Component Reaction ◽  
Key Steps ◽  
Modes Of Interaction ◽  
Native Ligand

A series of novel naphthopyrano[2,3-d]pyrimidin-11(12H)-one containing isoxazole nucleus 4 was synthesized under microwave irradiation and classical conditions in moderate to excellent yields upon 1,3-dipolar cycloaddition reaction using various arylnitrile oxides under copper(I) catalyst. A one-pot, three-component reaction, N-propargylation and Dimroth rearrangement were used as the key steps for the preparation of the dipolarophiles3. The structures of the synthesized compounds were established by 1H NMR, 13C NMR and HRMS-ES means. The present study aims to also predict the theoretical assembly of the COVID-19 protease (SARS-CoV-2 Mpro) and to discover in advance whether this protein can be targeted by the compounds 4a–1 and thus be synthesized. The docking scores of these compounds were compared to those of the co-crystallized native ligand inhibitor (N3) which was used as a reference standard. The results showed that all the synthesized compounds (4a–l) gave interesting binding scores compared to those of N3 inhibitor. It was found that compounds 4a, 4e and 4i achieved greatly similar binding scores and modes of interaction than N3, indicating promising affinity towards SARS-CoV-2 Mpro. On the other hand, the derivatives 4k, 4h and 4j showed binding energy scores (−8.9, −8.5 and −8.4 kcal/mol, respectively) higher than the Mpro N3 inhibitor (−7.0 kcal/mol), revealing, in their turn, a strong interaction with the target protease, although their interactions were not entirely comparable to that of the reference N3.

Antimycobacterial assessment and Microwave-assisted synthesis of 2-aryl-3-(4-methylphenylamino)thiazolidin-4-one derivatives

2021 ◽  
Vol 18 ◽  
Author(s):  
Saad Alghamdi ◽  
Mehnaz Kamal ◽  
Mohammad Asif
Keyword(s):  
Inhibitory Concentration ◽  
Aromatic Aldehydes ◽  
Microwave Assisted Synthesis ◽  
Alamar Blue ◽  
Mycobacterium Tuberculosis H37rv ◽  
Lead Compounds ◽  
Microwave Assisted ◽  
H37rv Strain ◽  
Antimycobacterial Agents

: This article reports the microwave-assisted synthesis, characterization, and evaluation of some -4-one derivatives (2a-2h) for their in-vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv strain by microplate Alamar blue assay (MABA) method. All these final compounds (2a-2h) were synthesized from Schiff’s bases, 1-arylidene-2-(4-methylphenyl)hydrazines (1a-1h), and thioglycolic acid by using zinc chloride as a catalyst. Compounds (1a-1h) were synthesized from the reaction of 4-methylhydrazine and appropriate aromatic aldehydes by Schiff’s reaction. Among the target compounds, 2-(4-ethoxyphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2f) and 2-(4-ethylphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2g) were promising with a minimum inhibitory concentration (MIC) of 12.5 μg/mL against M. tuberculosisH37Rv. Based on the preliminary results, compounds 2f and 2g were considered as lead compounds for the advanced design and development of antimycobacterial agents.

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