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 language | English (US) |
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Pages (from-to) | 2198-205 |
Number of pages | 8 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 26 |
Issue number | 9 |
DOIs | |
State | Published - May 1 2016 |
Keywords
- Journal Article
- Research Support, Non-U.S. Gov't