Synthesis and molecular modeling of antimicrobial active fluoroquinolone-pyrazine conjugates with amino acid linkers

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30 Scopus citations

Abstract

Novel fluoroquinolone-pyrazine conjugates 7a-h with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antimicrobial bioassay showed that the synthesized bis-conjugates have antimicrobial properties comparable to the parent drugs. Compound 7h showed superior antibacterial activity against Staphylococcus aureus and Streptococcus pyogenes (MIC=74.6 μM and 149.3 μM, respectively). This matched well with the estimated values obtained from 3D-pharmacophore and 2D-QSAR studies (MIC=67 μM and 92.9 μM, respectively).

Original languageEnglish (US)
Pages (from-to)2198-205
Number of pages8
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number9
DOIs
StatePublished - May 1 2016

Keywords

  • Journal Article
  • Research Support, Non-U.S. Gov't

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