simocyclinone-d8 and Escherichia-coli-Infections

simocyclinone-d8 has been researched along with Escherichia-coli-Infections* in 1 studies

Other Studies

1 other study(ies) available for simocyclinone-d8 and Escherichia-coli-Infections

ArticleYear
Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors.
    Bioorganic & medicinal chemistry letters, 2013, Nov-01, Volume: 23, Issue:21

    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.

    Topics: Anti-Bacterial Agents; Coumarins; DNA Gyrase; Escherichia coli; Escherichia coli Infections; Flavones; Glycosides; Humans; Models, Molecular; Topoisomerase II Inhibitors

2013