Synthesis and antibacterial evaluation of oxazolidin-2-ones structurally related to linezolid

Alessandra Ammazzalorso; Rosa Amoroso; Giancarlo Bettoni; Marialuigia Fantacuzzi; Barbara De Filippis; Letizia Giampietro; Cristina Maccallini; Domenico Paludi; Maria L Tricca

doi:10.1016/j.farmac.2004.05.002

Synthesis and antibacterial evaluation of oxazolidin-2-ones structurally related to linezolid

Farmaco. 2004 Sep;59(9):685-90. doi: 10.1016/j.farmac.2004.05.002.

Authors

Alessandra Ammazzalorso¹, Rosa Amoroso, Giancarlo Bettoni, Marialuigia Fantacuzzi, Barbara De Filippis, Letizia Giampietro, Cristina Maccallini, Domenico Paludi, Maria L Tricca

Affiliation

¹ Department of Drug Sciences, University of Chieti, via dei Vestini, 66100 Chieti, Italy.

PMID: 15337433
DOI: 10.1016/j.farmac.2004.05.002

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetamides / chemical synthesis*
Acetamides / pharmacology
Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / pharmacology
Drug Evaluation, Preclinical / methods
Humans
Linezolid
Microbial Sensitivity Tests / statistics & numerical data
Oxazolidinones / chemical synthesis*
Oxazolidinones / pharmacology
Staphylococcus / drug effects
Staphylococcus / growth & development
Structure-Activity Relationship

Substances

Acetamides
Anti-Bacterial Agents
Oxazolidinones
Linezolid