4.5 Article

Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl) fluoroquinolone derivatives containing an oxime functional moiety

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 9, Pages 2262-2267

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.050

Keywords

Fluoroquinolone derivatives; Synthesis; Antimycobacterial activity; Antibacterial activity

Funding

  1. National S&T Major Special Project on Major New Drug Innovations [2014ZX09507009-003]
  2. NSFC [81373267-003]
  3. Beijing Municipal Administration of Hospitals Clinical Medicine Development [ZYLX201304]

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A series of novel 1-(6-amino-3,5-difluoropyridin-2-yl) fluoroquinolone derivatives containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that compounds 9a-9c have considerable activity against both of MTB H37Rv ATCC 27294 (MICs: 3.81-7.13 mu g/mL) and methicillin-sensitive Staphylococcus aureus strains (MICs: <0.008-0.5 mu g/mL). (C) 2016 Elsevier Ltd. All rights reserved.

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