NDLI: Defining a minimum pharmacophore for simocyclinone D8 disruption of DNA gyrase binding to DNA

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Defining a minimum pharmacophore for simocyclinone D8 disruption of DNA gyrase binding to DNA

Content Provider	Springer Nature Link
Author	Gaskell, Lauren M. Nguyen, Thuy Ellis, Keith C.
Copyright Year	2014
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 used a deconstruction-reconstruction approach to prepare analogs of the coumarin subunit of SD8 and evaluated their ability to disrupt binding of the DNA gyrase enzyme to DNA in a surface plasmon resonance assay. This has led to a minimum pharmacophore required for disruption of binding.
Starting Page	3632
Ending Page	3643
Page Count	12
File Format	PDF
ISSN	10542523
Journal	Medicinal Chemistry Research
Volume Number	23
Issue Number	8
e-ISSN	15548120
Language	English
Publisher	Springer US
Publisher Date	2014-02-20
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Simocyclinone D8 DNA gyrase Antibiotics Natural product Catalytic inhibition Pharmacology/Toxicology Biochemistry Cell Biology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology, Toxicology and Pharmaceutics

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