Novel terpyridines as Staphylococcus aureus gyrase inhibitors: efficient synthesis and antibacterial assessment via solvent-drop grinding.
Mahmoud Abdalla MohamedAmr Salah AbouziedAmany ReyadMagdi E A ZakiFathy Elsayed AbdelgawadJehan Yahya Al-HumaidiSobhi Mohamed GomhaPublished in: Future medicinal chemistry (2024)
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.
Keyphrases
- molecular docking
- staphylococcus aureus
- silver nanoparticles
- bacillus subtilis
- multidrug resistant
- molecular dynamics simulations
- biofilm formation
- ionic liquid
- anti inflammatory
- escherichia coli
- pseudomonas aeruginosa
- human health
- cancer therapy
- single molecule
- circulating tumor
- acinetobacter baumannii
- risk assessment
- gram negative
- drug delivery
- case control
- wound healing
- machine learning
- artificial intelligence
- klebsiella pneumoniae
- nucleic acid
- candida albicans