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Bioorg Med Chem Lett ; 13(23): 4179-86, 2003 Dec 01.
Article in English | MEDLINE | ID: mdl-14622997

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Gram-Positive Bacteria/drug effects , Heterocyclic Compounds/chemistry , Methane/analogs & derivatives , Methane/chemistry , Oxazolidinones/chemical synthesis , Oxazolidinones/pharmacology , Staphylococcal Infections/drug therapy , Animals , Anti-Bacterial Agents/chemistry , Hydrocarbons , Mice , Microbial Sensitivity Tests , Oxazolidinones/chemistry , Rats , Staphylococcus aureus/pathogenicity , Structure-Activity Relationship
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