Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share By
Synthesis and Docking Study of Novel 4-Thiazolidinone Derivatives As Anti-Gram-Positive and Anti-H. Pylori Agents Publisher Pubmed



Khomami A1 ; Rahimi M1 ; Tabei A1 ; Saniee P2 ; Mahboubi A3 ; Foroumadi A4 ; Koopaei NN1 ; Almasirad A1
Authors

Source: Mini-Reviews in Medicinal Chemistry Published:2019


Abstract

Background: Bacterial resistance to the available antibiotics is a life threatening issue and researchers are trying to find new drugs to overcome this problem. Amongst the different structural classes, thiazolidinone-4-one, as a new effective pharmacophore against various bacteria, has been introduced. Objective: A new series of 2-(5-(5-nitrothiophene-2-yl)-1,3,4-thiadiazole-2-ylimino)-5-arylidenethia-zolidin-4-one derivatives were designed and synthesized as new antibacterial agents. Method: Target compounds were synthesized during 5 steps and their in vitro antibacterial and anti-H. pylori activities were evaluated. The interaction of the most active derivatives with the probable targets was assessed by Auto Dock 4.2 Program. Results: The results showed that the most potent compounds, 18, 22 and 23, displayed antibacterial activity versus S.aureus, S.epidermidis, B.cereus and B.subtilis (MIC, 1.56-12.5 μg/mL) and none of the derivatives were active on tested Gram-negative bacteria. Compound 12 in all considered doses and compounds 10, and 27 had strong anti-H. pylori activity (inhibition zone >20 mm) in 25 μg disc. Docking studies determined suitable interactions and affinity of potent compounds with bacterial MUR B and H. pylori urease enzymes. Conclusion: According to the results most of the derivatives are effective anti-bacterial agents and docking evaluation confirmed their possible mechanisms of actions as MURB and Urease inhibitors. © 2019 Bentham Science Publishers.
Related Docs
View other Related Docs
1. New Antimicrobial Nitro Heteroaryl-1,3,4-Thiadiazole Derivatives Containing Piperazinyl Benzonitrile Moiety: Synthesis and in Silico Study, Journal of Computational Biophysics and Chemistry (2022)
2. Design, Synthesis, Docking Study and Urease Inhibitory Activity Evaluation of Novel 2-((5-Amino-1,3,4-Thiadiazol-2-Yl)Thio)-N-Arylacetamide Derivatives, Medicinal Chemistry Research (2021)
3. Synthesis of New 2-(5-(5-Nitrofuran-2-Yl)-1,3,4-Thiadiazol-2-Ylimino)Thiazolidin-4-One Derivatives As Anti-Mrsa and Anti-H. Pylori Agents, BMC Chemistry (2022)
Experts (# of related papers)
View all Related Experts
Alireza Foroumadi (10)
Massoud Amanlou (4)
Other Related Docs
4. Synthesis and in Vitro Anti-Bacterial Activity of 2-(5-Nitro-2-Heteroaryl)-1,3,4-Thiadiazole Derivatives, Journal of Sciences# Islamic Republic of Iran (2020)
5. Synthesis, Molecular Docking, and Biological Evaluation of Nitroimidazole Derivatives As Potent Urease Inhibitors, Medicinal Chemistry Research (2021)
6. Novel 5-(Nitrothiophene-2-Yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity Against Promastigote Stage of Leishmania Major, Iranian Journal of Pharmaceutical Research (2019)
7. Synthesis and Biological Evaluation of 2-Phenyl Benzothiazole Derivatives As Cytotoxic Agents, Journal of Sciences# Islamic Republic of Iran (2018)
8. Thiazole in the Targeted Anticancer Drug Discovery, Future Medicinal Chemistry (2019)
9. Novel Quinazolines Bearing 1,3,4-Thiadiazole-Aryl Urea Derivative As Anticancer Agents: Design, Synthesis, Molecular Docking, Dft and Bioactivity Evaluations, BMC Chemistry (2024)
10. Semi-Synthesis of Novel Thebaine Derivatives With Low Cytotoxicity and Their Antibacterial and Antihemolytic Properties, Medicinal Chemistry Research (2023)
11. New Thioxothiazolidinyl-Acetamides Derivatives As Potent Urease Inhibitors: Design, Synthesis, in Vitro Inhibition, and Molecular Dynamic Simulation, Scientific Reports (2023)
12. Novel Fluoroquinolones Analogues Bearing 4-(Arylcarbamoyl)Benzyl: Design, Synthesis, and Antibacterial Evaluation, Molecular Diversity (2023)
13. New Ciprofloxacin–Dithiocarbamate–Benzyl Hybrids: Design, Synthesis, Antibacterial Evaluation, and Molecular Modeling Studies, Research on Chemical Intermediates (2019)
14. New 7-Piperazinylquinolones Containing (Benzo[D]Imidazol-2-Yl)Methyl Moiety As Potent Antibacterial Agents, Molecular Diversity (2018)
15. Design and Synthesis of Tetrahydropyrimidinone(Thione)-Triazole Hybrid Scaffolds and Evaluation of Their Biological Activities, Phosphorus# Sulfur and Silicon and the Related Elements (2021)
16. Design, Synthesis and in Vitro Cytotoxicity of New 1,2,3-Triazol-And Nitrostyrene Hybrids As Potent Anticancer Agents, Letters in Drug Design and Discovery (2018)
17. Synthesis, Characterization and Biological Evaluation of Novel 3-Methyl-5-Pyrazolone Derivatives, Journal of Medicinal and Chemical Sciences (2021)
18. Thiosemicarbazone Derivatives Act As Potent Urease Inhibitors; Synthesis, Bioactivity Screening and Molecular Docking Study, ChemistrySelect (2022)
19. Recent Applications of 1,3-Thiazole Core Structure in the Identification of New Lead Compounds and Drug Discovery, European Journal of Medicinal Chemistry (2015)
20. Synthesis of Thiazolone Derivatives As Novel Soybean 15-Lox Inhibitors, Letters in Organic Chemistry (2017)