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Future Med Chem ; 16(3): 205-220, 2024 02.
Article in English | MEDLINE | ID: mdl-38230640

ABSTRACT

Aim: This study was designed to synthesize a novel series of terpyridines with potential antibacterial properties, targeting multidrug resistance. Materials & methods: Terpyridines (4a-h and 6a-c) were synthesized via a one-pot multicomponent reaction using 2,6-diacetylpyridines, benzaldehyde derivatives and malononitrile or ethyl 2-cyanoacetate. The reactions, conducted under grinding conditions with glacial acetic acid, produced high-yield compounds, confirmed by spectroscopic data. Results: The synthesized terpyridines exhibited potent antibacterial activity. Notably, compounds 4d and 4h demonstrated significant inhibition zones against Staphylococcus aureus and Bacillus subtilis, outperforming ciprofloxacin. Conclusion: Molecular docking studies highlighted compounds 4d, 4h and 6c as having strong binding affinity to DNA gyrase B, correlating with their robust antibacterial activity, suggesting their potential as effective agents against multidrug-resistant bacterial strains.


Subject(s)
Anti-Bacterial Agents , Staphylococcus aureus , Molecular Docking Simulation , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , DNA Gyrase/metabolism , Microbial Sensitivity Tests , Topoisomerase II Inhibitors/pharmacology , Topoisomerase II Inhibitors/chemistry , Structure-Activity Relationship , Molecular Structure
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