title: Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus.
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.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Naresh
authors.initials: N
authors.lastname: Sunduru
authors.forename: Leena
authors.initials: L
authors.lastname: Gupta
authors.forename: Kuldeep
authors.initials: K
authors.lastname: Chauhan
authors.forename: Nripendra N
authors.initials: NN
authors.lastname: Mishra
authors.forename: Praveen K
authors.initials: PK
authors.lastname: Shukla
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004347:Drug Interactions; D005449:Fluorenes / Q000737:chemistry*; D005464:Fluorobenzenes / Q000737:chemistry; D005493:Folic Acid Antagonists / Q000494:pharmacology; D007711:Klebsiella pneumoniae / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013762:Tetrahydrofolate Dehydrogenase / Q000378:metabolism; D020713:Vancomycin Resistance / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D005449:Fluorenes; D005464:Fluorobenzenes; D005493:Folic Acid Antagonists; C041509:fluorene; C044697:benzotrifluoride; D013762:Tetrahydrofolate Dehydrogenase; D009643:Norfloxacin