A branching synthetic strategy was used to efficiently generate structurally diverse scaffolds, which span a broad area of chemical descriptor space, and their biological activity against MRSA was demonstrated.
The screening of a diversity-oriented synthesis library followed by structure-activity relationship investigations have led to the discovery of an anti-MRSA agent which operates as an inhibitor of Staphylococcus aureus dihydrofolate reductase.
Cyclopropane derivatives Q 0021Skeletal Diversity Construction via a Branching Synthetic Strategy. -A strategy is described which starts from a fluorous-tagged two carbon unit, e.g. (I), and uses divergent, complexity-generating reaction pathways to create maximum skeletal diversity in the final products. A library of 223 small molecules is synthesized, which have 30 distinct molecular frameworks. -(WYATT, E. E.; FERGUS, S.; GALLOWAY, W. R. J. D.; BENDER, A.; FOX, D. J.; PLOWRIGHT, A. T.; JESSIMAN, A. S.; WELCH, M.; SPRING*, D. R.; Chem. Commun. (Cambridge) 2006, 31, 3296-3298; Dep. Chem., Univ. Cambridge, Cambridge CB2 1EW, UK; Eng.) -M. Paetzel 52-067
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