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

• Published in: Farmaco (Società chimica italiana : 1989) Vol. 59; no. 9; pp. 685 - 690
• Main Authors: Ammazzalorso, Alessandra, Amoroso, Rosa, Bettoni, Giancarlo, Fantacuzzi, Marialuigia, De Filippis, Barbara, Giampietro, Letizia, Maccallini, Cristina, Paludi, Domenico, Tricca, Maria L.
• Format: Journal Article
• Language: English
• Published: France Elsevier SAS 01-09-2004
• Subjects: Acetamides - chemical synthesis; Acetamides - pharmacology; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Antibacterial activity; Drug Evaluation, Preclinical - methods; Humans; Linezolid; Microbial Sensitivity Tests - statistics & numerical data; Oxazolidin-2-ones; Oxazolidinones - chemical synthesis; Oxazolidinones - pharmacology; Staphylococcus - drug effects; Staphylococcus - growth & development; Structure-Activity Relationship; Linezolid; Antibacterial activity; Oxazolidin-2-ones
• ISSN: 0014-827X; 1879-0569
• DOI: 10.1016/j.farmac.2004.05.002

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.