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  • Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus.

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 (2011-02-25)
Naresh Sunduru, Leena Gupta, Kuldeep Chauhan, Nripendra N Mishra, Praveen K Shukla, Prem M S Chauhan
ABSTRACT

A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives incorporated with 1,3,5-triazine and pyrimidine were synthesized. All the above compounds were evaluated for their antibacterial activity against Klebsiella pneumoniae, methicillin-resistant Staphylococcus aureus and methicillin & vancomycin-resistant S. aureus. Among all, compounds having Morpholine, N-methyl/phenyl/benzyl/pyrimidinyl piperazines and n-butylamine substitution at C-7 position, have shown increased potency in comparison to norfloxacin and ciprofloxacin.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
α,α,α-Trifluorotoluene, anhydrous, ≥99%
Sigma-Aldrich
α,α,α-Trifluorotoluene, ≥99%
Supelco
Ciprofloxacin, VETRANAL®, analytical standard
Supelco
Norfloxacin, analytical standard, ≥98% (TLC)
Sigma-Aldrich
Ciprofloxacin, ≥98% (HPLC)
Sigma-Aldrich
α,α,α-Trifluorotoluene solution, suitable for NMR (reference standard), 0.05% in benzene-d6 (99.6 atom % D)
Supelco
Norfloxacin, VETRANAL®, analytical standard