Synthesis and antibacterial evaluation of oxazolidin-2-ones structurally related to linezolid.
Compounds structurally related to the known antimicrobial drug linezolid were selected in order to evaluate the influence of electron-withdrawing properties and altered geometric features as a result of the N-substituent modification. After a preliminary study of molecular modeling, cinnamoyl-, pyridin- and pyrimidinoxazolidin-2-ones were synthesized. None of the new compounds showed antibacterial activity.
Ammazzalorso
Alessandra
A
Department of Drug Sciences, University of Chieti, via dei Vestini, 66100 Chieti, Italy.
Amoroso
Rosa
R
Bettoni
Giancarlo
G
Fantacuzzi
Marialuigia
M
De Filippis
Barbara
B
Giampietro
Letizia
L
Maccallini
Cristina
C
Paludi
Domenico
D
Tricca
Maria L
ML
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D000069349:Linezolid; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013210:Staphylococcus / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D000069349:Linezolid