4-Thiazolidinone derivatives as potent antimicrobial agents: microwave-assisted synthesis, biological evaluation and docking studies

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 319-326 ◽  
Author(s):  
Eleni Pitta ◽  
Evangelia Tsolaki ◽  
Athina Geronikaki ◽  
Jovana Petrović ◽  
Jasmina Glamočlija ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Activity ◽  
Antimicrobial Agents ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Hiv 1

A series of ten thiazolidin-4-one derivatives was synthesized and evaluated for their antibacterial, antifungal and HIV-1 reverse transcriptase (RT) inhibitory activity.

scholarly journals Microwave Assisted Synthesis of Quinoline Fused Benzodiazepines as Anxiolytic and Antimicrobial Agents

2021 ◽  
Vol 33 (5) ◽  
pp. 1107-1114
Author(s):  
S.B. Marganakop ◽  
R.R. Kamble ◽  
A.R. Nesaragi ◽  
P.K. Bayannavar ◽  
S.D. Joshi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Docking Studies ◽  
K Channel ◽  
Microwave Assisted Synthesis ◽  
Green Protocol ◽  
Microwave Assisted ◽  
Consensus Score ◽  
Surflex Docking

In the present study, an efficient, facile and green protocol for synthesis of quinoline fused 1,4-benzodiazepine (4a-j) by microwave irradiated condensation of 6/7/8-substituted 3-bromomethyl- 2-chloro-quinoline (3a-j) obtained from 2-chloro 6/7/8-substituted quinoline-3-carbaldehyde (1a-j) with 1, 2-phenylenediamine was developed. Surflex docking studies with K+ channel is one of the physiological targets and inhibition, which plays a role in the pathophysiology of depression revealed that all these compounds show consensus score in the range 2.71-3.68 indicating the summary of all forces of interaction. Further, compounds 4d, 4g and 4i exhibited potent antibacterial activity

scholarly journals Microwave-assisted synthesis, biological evaluation and molecular docking studies of new coumarin-based 1,2,3-triazoles

RSC Advances ◽  
2020 ◽  
Vol 10 (20) ◽  
pp. 11615-11623 ◽  
Author(s):  
Ravinder Dharavath ◽  
Nalaparaju Nagaraju ◽  
M. Ram Reddy ◽  
D. Ashok ◽  
M. Sarasija ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Click Reaction ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Microwave Assisted Synthesis ◽  
Terminal Alkynes ◽  
Triazole Derivatives ◽  
Molecular Docking Studies ◽  
Microwave Assisted ◽  
Highly Efficient

Coumarin-based 1,4-disubstituted 1,2,3-triazole derivatives were synthesized using a highly efficient, eco-friendly protocol via a copper(i)-catalyzed click reaction between various substituted arylazides and terminal alkynes.

Microwave assisted synthesis and biological evaluation of a series of 1,5-benzothiazepines as potential cytotoxic and antimicrobial agents

2014 ◽  
Vol 5 (1) ◽  
pp. 138-143 ◽  
Author(s):  
Subhash Yenupuri ◽  
Agastyaraju V. L. N. Satyanarayana Hariharan ◽  
Bharat Kumar Bugata ◽  
Divakara Laxman Somayajulu Nori
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Synthesis And Biological Evaluation

scholarly journals Novel Thiazolidin-4-ones as Potential Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3821 ◽  
Author(s):  
Petrou ◽  
Eleftheriou ◽  
Geronikaki ◽  
Akrivou ◽  
Vizirianakis
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Activity ◽  
Inhibitory Action ◽  
Docking Studies ◽  
Prediction Program ◽  
Ic50 Values ◽  
Acquired Immunodeficiency ◽  
Hiv Drugs ◽  
Immunodeficiency Syndrome ◽  
Hiv 1

Background: HIV is the causative agent of Acquired Immunodeficiency Syndrome (AIDS), an infectious disease with increasing incidence worldwide. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) play an important role in the treatment of AIDS. Although, many compounds are already being used as anti-HIV drugs, research for the development of new inhibitors continues as the virus develops resistant strains. Methods: The best features of available NNRTIs were taken into account for the design of novel inhibitors. PASS (Prediction of activity spectra for substances) prediction program and molecular docking studies for the selection of designed compounds were used for the synthesis. Compounds were synthesized using conventional and microwave irradiation methods and HIV RT inhibitory action was evaluated by colorimetric photometric immunoassay. Results: The evaluation of HIV-1 RT inhibitory activity revealed that seven compounds have significantly lower ΙC50 values than nevirapine (0.3 μΜ). It was observed that the activity of compounds depends not only on the nature of substituent and it position in benzothiazole ring but also on the nature and position of substituents in benzene ring. Conclusion: Twenty four of the tested compounds exhibited inhibitory action lower than 4 μΜ. Seven of them showed better activity than nevirapine, while three of the compounds exhibited IC50 values lower than 5 nM. Two compounds 9 and 10 exhibited very good inhibitory activity with IC50 1 nM.

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.

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