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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity
Richard M Beteck1, Audrey Jordaan2, Tarryn Swart3
1Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
Abstract:
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.
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