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Bioorg Med Chem Lett. 2013 Nov 1;23(21):5874-7. doi: 10.1016/j.bmcl.2013.08.094. Epub 2013 Sep 5.

Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors.

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Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Biotech 1, 800 East Leigh Street, Richmond, VA 23298, USA.


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.


Antibiotics; DNA gyrase; Flavone; Natural product; Quercetin; Simocyclinone D8

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