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Oxazolidinone Structure–Activity Relationships Leading to Linezolid
Author(s) -
Barbachyn Michael R.,
Ford Charles W.
Publication year - 2003
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200200528
Subject(s) - linezolid , antimicrobial , multiple drug resistance , identification (biology) , antibiotic resistance , pathogen , broad spectrum , antibacterial activity , antibiotics , medicine , intensive care medicine , biology , staphylococcus aureus , microbiology and biotechnology , bacteria , chemistry , combinatorial chemistry , botany , vancomycin , genetics
The development of bacterial resistance to currently available antibacterial agents is a growing global health problem. Of particular concern are infections caused by multidrug‐resistant Gram‐positive pathogens which are responsible for significant morbidity and mortality in both the hospital and community settings. A number of solutions to the problem of bacterial resistance are possible. The most common approach is to continue modifying existing classes of antibacterial agents to provide new analogues with improved attributes. Other successful strategies are to combine existing antibacterial agents with other drugs as well as the development of improved diagnostic procedures that may lead to rapid identification of the causative pathogen and permit the use of antibacterial agents with a narrow spectrum of activity. Finally, and most importantly, the discovery of novel classes of antibacterial agents employing new mechanisms of action has considerable promise. Such agents would exhibit a lack of cross‐resistance with existing antimicrobial drugs. This review describes the work leading to the discovery of linezolid, the first clinically useful oxazolidinone antibacterial agent.