Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 22, Pages 5058-5063Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.10.027
Keywords
Fluoroquinolone derivatives; Synthesis; Antimycobacterial activity; Antibacterial activity
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Funding
- National S&T Major Special Project on Major New Drug Innovations [2012ZX09301002-001-017/023, 2014ZX09507009-003]
- NSFC [81373267-003]
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A series of novel 1-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives 21-24 containing an oxime-functionalized pyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results reveal that compounds 21a, 21e and 21j show considerable activity against MTB H37Rv ATCC 27294 (MICs: <0.25 mu g/mL) and MDR-MTB 6133 (MICs: 0.03-0.054 lg/mL). The target compounds 21-24 are generally poor against the Gram-negative strains, but 21a-j and 22a-c have potent potency (MICs: <0.008-32 mu g/mL) against all of the tested Gram-positive strains including MRSA and MRSE with a few exceptions, and the most active compounds 21d, 21e and 22a-c (MICs: <0.008-32 mu g/mL) were found to be comparable to or better than moxifloxacin, and 2->250 times more potent than ciprofloxacin and levofloxacin. (C) 2015 Elsevier Ltd. All rights reserved.
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