Synthesis and evaluation of urea and thiourea derivatives of oxazolidinones as antibacterial agents.
Urea and thiourea derivatives of oxazolidinones were synthesized and their inhibitory activity (MIC) was determined on the bacterial strains which includes clinical isolates and quality control organisms. The structure activity relationships were studied and a 3D-QSAR model was built using Genetic Function Approximation. Interestingly found that electron withdrawing groups at the ortho position of the phenyl ring enhances the activity.
Aaramadaka
Sunil Kumar Reddy
SK
New Drug Discovery, Orchid Chemicals & Pharmaceuticals Ltd., Chennai, Tamilnadu, India. sunil@scientist.com
Guha
Mrinal Kanthi
MK
Prabhu
Ganesh
G
Kini
Suvarna Ganesh
SG
Vijayan
Magesh
M
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D013293:Enterococcus faecalis / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship; D013210:Staphylococcus / Q000187:drug effects*; D013890:Thiourea / Q000737:chemistry*; D014508:Urea / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D014508:Urea; D013890:Thiourea