Design and synthesis of new N-substituted amino methyl-[1,2,3] triazolyl moieties of fluoroquinolones as antibacterial agents

Medicinal Chemistry Research
2013.0

Abstract

A series of twenty new N-substituted amino methyl-[1,2,3] triazolyl derivatives at C-7 position of fluoroquinolones were designed and synthesized through multistep synthesis. The synthesized compounds were characterized by 1 H NMR, 13C NMR, ESI–MS, and IR. The antibacterial activities of these new fluoroquinolones were evaluated using a standard broth micro dilution technique. Out of the twenty derivatives, aryl substituted amino derivatives (6m to 6q) exhibited very good potency in inhibiting the growth of Methicillin-sensitive Staphylococcus aureus (MSSA), Methicillin-resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococcus faecalis (VRE faecalis) (MIC: 0.25–4.00 lg/mL) as compared to the marketed drugs Linezolid and Ciprofloxacin.

Knowledge Graph

Similar Paper

Design and synthesis of new N-substituted amino methyl-[1,2,3] triazolyl moieties of fluoroquinolones as antibacterial agents
Medicinal Chemistry Research 2013.0
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone derivatives
Bioorganic & Medicinal Chemistry Letters 2011.0
4-Substituted 4-(1H-1,2,3-triazol-1-yl)piperidine: Novel C7 moieties of fluoroquinolones as antibacterial agents
Bioorganic & Medicinal Chemistry Letters 2010.0
Synthesis and in vitro antibacterial activity of 7-(3-Alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives
European Journal of Medicinal Chemistry 2011.0
Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives
Bioorganic & Medicinal Chemistry Letters 2011.0
Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus
European Journal of Medicinal Chemistry 2011.0
A new efficient route to 7-aryl-6-fluoro-8-nitroquinolones as potent antibacterial agents
European Journal of Medicinal Chemistry 2014.0
Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives
Journal of Medicinal Chemistry 1989.0
Synthesis and structure-activity relationships of novel arylfluoroquinolone antibacterial agents
Journal of Medicinal Chemistry 1985.0
Synthesis and antibacterial activity of novel fluoroquinolones containing substituted piperidines
Bioorganic & Medicinal Chemistry Letters 2007.0