ABSTRACT
A series of pyrrolopyridine-substituted oxazolidinones containing various C-5 acetamide isosteres was synthesized and the structure-antibacterial activity relationships determined against a representative panel of susceptible and resistant Gram-positive bacteria.
Subject(s)
Acetamides/chemistry , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Oxazolidinones/chemistry , Oxazolidinones/pharmacology , Pyridines/chemistry , Anti-Bacterial Agents/chemistry , Enterococcus/drug effects , Linezolid , Molecular Structure , Oxazolidinones/chemical synthesis , Staphylococcus aureus/drug effects , Structure-Activity RelationshipABSTRACT
A series of oxazolidinone antibacterial agents containing a 5-substituted isoxazol-3-yl moiety were synthesized via a nitrile oxide [3+2] dipolar cycloaddition reaction. These compounds were screened against a panel of susceptible and resistant Gram-positive organisms. Several analogs from this series were comparable to or more potent than linezolid in vitro.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Isoxazoles/chemical synthesis , Oxazolidinones/chemical synthesis , Animals , Anti-Bacterial Agents/pharmacology , Drug Evaluation, Preclinical/methods , Female , Isoxazoles/pharmacology , Mice , Microbial Sensitivity Tests/methods , Oxazolidinones/pharmacologyABSTRACT
A novel series of oxazolidinones containing a pyrroloaryl substituent was synthesized and screened against a representative panel of susceptible and resistant Gram-positive bacteria. Several members of this series were found to have antibacterial activity comparable to or better than linezolid.
