Synthesis and antimicrobial activity of 2,3-bis(bromomethyl)quinoxaline derivatives

We synthesized 12 derivatives of 2,3-bis(bromomethyl)quinoxaline with substituents at the 6- and/or 7-positions, and evaluated their activities against bacteria and fungi. Of the 12 compounds, nine (1a-h, 1j, and 1k) showed antibacterial activity. The derivative 1g, which bears a trifluoromethyl group at the 6-position, showed the highest activity against Gram-positive bacteria, while 1c, which has a fluoro-group at the 6-position, showed the widest antifungal activity spectrum. However, only the derivative with an ethyl ester substitution, 1k showed activity against Gram-negative bacteria.

Twelve 2,3-bis(bromomethyl)quinoxaline derivatives were synthesized and screened for antibacterial and antifungal activities.Figure optionsDownload as PowerPoint slideHighlights
► Novel 2,3-bis(bromomethyl)quinoxaline derivatives were synthesized.
► Their antibacterial and antifungal activities have been reported.
► 6-(Trifluoromethyl)-2,3-bis(bromomethyl)quinoxaline had the highest antibacterial activity.
► 6-Fluoro-2,3-bis(bromomethyl)quinoxaline showed the widest antifungal activity spectrum.