Anti-MRSA Agent Discovery Using Diversity-Oriented Synthesis (pages 2808–2812)
Gemma L. Thomas, Richard J. Spandl, Freija G. Glansdorp, Martin Welch, Andreas Bender, Joshua Cockfield, Jodi A. Lindsay, Clare Bryant, Derek F. J. Brown, Olivier Loiseleur, Hélène Rudyk, Mark Ladlow and David R. Spring
Article first published online: 28 FEB 2008 | DOI: 10.1002/anie.200705415
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).