New azetidine-3-carbonyl-N-methyl-hydrazino derivatives of fluoroquinolones: synthesis and evaluation of antibacterial and anticancer properties
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Date
2014
Journal Title
Journal ISSN
Volume Title
Publisher
Medicinal Chemistry Research
Abstract
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 1H NMR, 13C 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 lg/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.
Description
Keywords
Synthesis, Reductive amination, Fluoroquinolones, Antibacterial activity, Anticancer activity
Citation
Rajulu, G. G., Naik, H. S. B., Kumar, G. C., Ramaraj, S., Sambasivam, G., & Koppolu, K. P. (2014). New azetidine-3-carbonyl-N-methyl-hydrazino derivatives of fluoroquinolones: synthesis and evaluation of antibacterial and anticancer properties. Medicinal Chemistry Research, 23, 2856-2868. 10.1007/s00044-013-0873-0