New library of pyrazole-imidazo[1,2-α]pyridine molecular conjugates: Synthesis, antibacterial activity and molecular docking studies.
Oluwakemi EbenezerPaul AwoladeNeil KoorbanallyParvesh SinghPublished in: Chemical biology & drug design (2019)
A library of novel pyrazole-imidazo[1,2-α]pyridine scaffolds was designed and synthesized through a one-pot three-component tandem reaction. The structures of synthesized conjugates were confirmed by spectroscopic techniques (NMR, IR and HRMS). In vitro antibacterial evaluation of the twelve synthesized molecules (7a, 8a-k) against methicillin-resistant Staphylococcus aureus and normal strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumonia and Pseudomonas aeruginosa established 8b, 8d, 8e, 8h and 8i as potent antibacterial agents with superior minimum bactericidal concentration, compared with standard drug ciprofloxacin. Molecular docking studies of all active compounds into the binding site of glucosamine-6-phosphate synthase were further performed in order to have a comprehensive understanding of putative binding modes within the active sites of the receptor.
Keyphrases
- molecular docking
- escherichia coli
- methicillin resistant staphylococcus aureus
- pseudomonas aeruginosa
- silver nanoparticles
- molecular dynamics simulations
- biofilm formation
- high resolution
- staphylococcus aureus
- case control
- cystic fibrosis
- listeria monocytogenes
- magnetic resonance
- oxide nanoparticles
- cancer therapy
- klebsiella pneumoniae
- acinetobacter baumannii
- binding protein
- anti inflammatory
- dna binding
- high resolution mass spectrometry
- transcription factor
- intensive care unit
- essential oil
- adverse drug
- solid state