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Synthesis of novel oxazolidinone antimicrobial agents.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Mar 01; Vol. 16 (5), pp. 2651-6. Date of Electronic Publication: 2007 Nov 19. - Publication Year :
- 2008
-
Abstract
- The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 microg/mL, which is comparable to the well-known oxazolidinone, linezolid.
- Subjects :
- Anti-Bacterial Agents chemistry
Escherichia coli drug effects
Molecular Structure
Oxazolidinones chemistry
Staphylococcus aureus drug effects
Structure-Activity Relationship
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents pharmacology
Oxazolidinones chemical synthesis
Oxazolidinones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 16
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 18077175
- Full Text :
- https://doi.org/10.1016/j.bmc.2007.11.040