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Article: Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors
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Article co-written by Northwestern Health Sciences University faculty member Lisa Oppegard. The article was published in Bioorganic and Medicinal Chemistry Letters and was made available online by Elsevier in 2013. Citation: Volume 23, Issue 21, November 2013, Pages 5874-5877.
Abstract
The increasing occurrence of drug-resistant bacterial infections in the clinic has created a need for new antibacterial agents. Natural products have historically been a rich source of both antibiotics and lead compounds for new antibacterial agents. The natural product simocyclinone D8 (SD8) has been reported to inhibit DNA gyrase, a validated antibacterial drug target, by a unique catalytic inhibition mechanism of action. In this work, we have prepared simplified flavone-based analogues inspired by the complex natural product and evaluated their inhibitory activity and mechanism of action. While two of these compounds do inhibit DNA gyrase, they do so by a different mechanism of action than SD8, namely DNA intercalation.