Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 23, Issue 6, Pages 2856-2868Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-013-0873-0
Keywords
Synthesis; Reductive amination; Fluoroquinolones; Antibacterial activity; Anticancer activity
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A series of nine new N-(substituted azetidine-3-carbonyl)-N-methyl-hydrazino derivatives at C-7 position of fluoroquinolones were designed and synthesized through multistep synthesis. The synthesized compounds were characterized by H-1 NMR, C-13 NMR, ESI-MS and IR. The new compounds were tested for their in vitro antimicrobial and anti-proliferative activity. Out of the nine derivatives, compound 6i exhibited good antibacterial activity by inhibiting the growth of Methicillin-sensitive Staphylococcus aureus, Methicillin-resistant S. aureus and ATCC 35218 Escherichia coli (MIC: 0.25-16.00 mu g/mL). Compounds 6c, 6g-h are displayed good growth inhibition against MCF-7 Breast carcinoma, HCT-116 Colon carcinoma and A549 Lung adenocarcinoma cell lines. Compound 6h is the most active against MCF-7 cell line with superior growth inhibition compared to ciprofloxacin and reference anticancer drug SAHA.
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