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Synthesis, antimycobacterial and antibacterial activity of ciprofloxacin derivatives containing a N-substituted benzyl moiety.

Abstract：

:We report herein the design and synthesis of a series of novel ciprofloxacin (CPFX) derivatives with remarkable improvement in lipophilicity by introducing a substituted benzyl moiety to the N atom on the C-7 piperazine ring of CPFX. Antimycobacterial and antibacterial activity of the newly synthesized compounds was evaluated. Results reveal that compound 4f has good in vitro activity against all of the tested Gram-positive strains including MRSA and MRSE (MICs: 0.06-32 μg/mL) which is two to eightfold more potent than or comparable to the parent drug CPFX (MICs: 0.25-128 μg/mL), Gram-negative bacteria P. aeruginosa (MICs: 0.5-4 μg/mL) and M. tuberculosis H37Rv ATCC 27294 (MIC: 1 μg/mL).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wang S,Jia XD,Liu ML,Lu Y,Guo HY

doi

10.1016/j.bmcl.2012.07.040

subject

Has Abstract

pub_date

2012-09-15 00:00:00

pages

5971-5

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00916-X

journal_volume

22

pub_type

杂志文章

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