Anti-MRSA Agent Discovery Using Diversity-Oriented Synthesis

Beating the superbugs: Diversity‐oriented synthesis using a solid‐supported phosphonate unit to synthesize 242 drug‐like compounds based on 18 natural‐product‐like scaffolds led to the discovery of gemmacin (see scheme). This new structural class of antibiotic is active towards methicillin‐resistant...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2008-03, Vol.47 (15), p.2808-2812
Main Authors: Thomas, Gemma L., Spandl, Richard J., Glansdorp, Freija G., Welch, Martin, Bender, Andreas, Cockfield, Joshua, Lindsay, Jodi A., Bryant, Clare, Brown, Derek F. J., Loiseleur, Olivier, Rudyk, Hélène, Ladlow, Mark, Spring, David R.
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
antibiotics
combinatorial chemistry
diversity-oriented synthesis
Drug Evaluation, Preclinical - methods
Methicillin Resistance
Molecular Structure
Staphylococcus aureus - drug effects
Staphylococcus aureus - physiology
synthesis design
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Summary:Beating the superbugs: Diversity‐oriented synthesis using a solid‐supported phosphonate unit to synthesize 242 drug‐like compounds based on 18 natural‐product‐like scaffolds led to the discovery of gemmacin (see scheme). This new structural class of antibiotic is active towards methicillin‐resistant Staphylococcus aureus (MRSA).
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200705415