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One-Pot Synthesis of 5-(Het)Aryl 8-Aminoquinoline Amide Derivatives as Potential Antibacterial / Cytotoxic Agents


Zanjam Spandana, T. Malathi Rekha, Mandava V. Basaveswara Rao and Manojit Pal*   Pages 1 - 9 ( 9 )


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 Gram-(


Quinolone, suzuki-miyaura coupling, Pd/C, antibacterial activity, cytotoxicity.


Krishna University, Machilipatnam-521001, Department of Chemistry, SPHM Kalasala, Machilipatnam-521001, Department of Chemistry, Krishna University, Machilipatnam-521001, Department of Chemistry, Dr. Reddy`s Institute of Life Sciences, Organic and Medicinal Chemistry, University of Hyderabad Campus

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