Background: The 8-aminoquinoline (8-AQ) framework has attracted particular attention in
the discovery and development of antimalarial and anti-bacterial agents or drugs. However, the clinical
uses of 8-AQ based drugs are often associated with toxic side effects such as methemoglobinemia and
hemolytic anemia with deficiency in glucose-6-phosphate dehydrogenase (G6PD) activity. The 4-aryl-
8-amino(acetamido)quinoline derivatives, on the other hand, have shown antiproliferative activities
against cancer cell lines. These reports prompted us to assess the antibacterial and cytotoxic activities of
a series of compounds based on 5-aryl 8-aminoquinoline amide scaffold.
Methods: A series of compounds based on 5-(het)aryl 8-aminoquinoline amide scaffold was synthesized
via a one-pot ultrasound-assisted method using a C-5 selective halogenation of quinoline derivatives
followed by Pd/C-catalyzed Suzuki-Miyaura coupling with (het)aryl boronic acids. All these
compounds were evaluated for their in vitro antibacterial activities against representative Gram-(+) and
Keywords: Quinolone, suzuki-miyaura coupling, Pd/C, antibacterial activity, cytotoxicity.
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