期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 21, 页码 5874-5877出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.094
关键词
Simocyclinone D8; DNA gyrase; Antibiotics; Natural product; Flavone; Quercetin
资金
- VCU/MCV A.D. Williams Trust Fund
- Thomas F. and Kate Miller Jeffress Memorial Trust Fund
- VCU School of Pharmacy
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. (C) 2013 Elsevier Ltd. All rights reserved.
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