1469894-72-1Relevant articles and documents
Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors
Verghese, Jenson,Nguyen, Thuy,Oppegard, Lisa M.,Seivert, Lauren M.,Hiasa, Hiroshi,Ellis, Keith C.
, p. 5874 - 5877 (2013/10/22)
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.