6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity.
Richard M BeteckAudrey JordaanTarryn SwartFrank Van Der KooyDigby F WarnerHeinrich C HoppeLesetja J LegoabePublished in: Chemical biology & drug design (2020)
In this study, we synthesized novel nitro quinolone-based compounds and tested them in vitro against a panel of Gram-positive and Gram-negative pathogens including Mycobacterium tuberculosis (MTB), Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumonia, Staphylococcus aureus, and Escherichia coli for antibacterial activities and also against HeLa cells for overt cytotoxicity. Compound 8e was identified as a non-toxic, potent hit with selective activity (MIC90 ˂ 0.24 µm) against MTB. 8e, however, showed no activity against DprE1 mutant, suggesting DprE1 as the likely target for this compound class.
Keyphrases
- gram negative
- multidrug resistant
- acinetobacter baumannii
- mycobacterium tuberculosis
- pseudomonas aeruginosa
- drug resistant
- escherichia coli
- staphylococcus aureus
- pulmonary tuberculosis
- klebsiella pneumoniae
- biofilm formation
- induced apoptosis
- cell cycle arrest
- cystic fibrosis
- cell proliferation
- anti inflammatory
- oxidative stress
- signaling pathway
- candida albicans
- acute respiratory distress syndrome
- extracorporeal membrane oxygenation
- oxide nanoparticles