Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587278 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
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.
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Authors
Jenson Verghese, Thuy Nguyen, Lisa M. Oppegard, Lauren M. Seivert, Hiroshi Hiasa, Keith C. Ellis,