New classes of antibacterial oxazolidinones with C-5, methylene O-Linked heterocyclic side chains

Exploration of the structure–activity relationships of the traditional C-5 acetamidomethyl side chain of the oxazolidonone antibacterials has yielded new, potent series of compounds of which the first examples, the O-linked iosoxazoles are described in detail, leading to the selection of the pre-cli...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-12, Vol.13 (23), p.4179-4186
Hauptverfasser:	Gravestock, Michael B, Acton, David G, Betts, Michael J, Dennis, Michael, Hatter, Glenn, McGregor, Alexandra, Swain, Michael L, Wilson, R.Geoffrey, Woods, Lisa, Wookey, Alan
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Gram-Positive Bacteria - drug effects Heterocyclic Compounds - chemistry Hydrocarbons Methane - analogs & derivatives Methane - chemistry Mice Microbial Sensitivity Tests Oxazolidinones - chemical synthesis Oxazolidinones - chemistry Oxazolidinones - pharmacology Rats Staphylococcal Infections - drug therapy Staphylococcus aureus - pathogenicity Structure-Activity Relationship
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Zusammenfassung:	Exploration of the structure–activity relationships of the traditional C-5 acetamidomethyl side chain of the oxazolidonone antibacterials has yielded new, potent series of compounds of which the first examples, the O-linked iosoxazoles are described in detail, leading to the selection of the pre-clinical candidate AZD2563. Novel potent oxazolidinone antibacterials with heterocyclic C-5 side chains are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.07.033