216869-07-7Relevant articles and documents
Photochemistry of oxazolidinone antibacterial drugs
Fasani, Elisa,Tilocca, Fedele,Albini, Angelo
experimental part, p. 879 - 885 (2010/02/28)
The photochemistry of six N3-(3-fluoro-4-dialkylaminophenyl)-oxazolidinones known for their antimicrobial activity has been examined. All of these compounds are defluorinated in water (φdec ≈ 0.25) and in methanol (φdec ≈ 0.03), reas
Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 3.1) Synthesis and evaluation of 5-thiocarbamate oxazolidinones
Tokuyama,Takahashi,Tomita,Tsubouchi,Iwasaki,Kado,Okezaki,Nagata
, p. 361 - 367 (2007/10/03)
A series of 5-thiocarbamate oxazolidinones was prepared and tested for in vitro and in vivo antibacterial activities. The results of in vitro antibacterial activity indicated that the 5-thiocarbamate group was a suitable substituent for the activity by the 5-moderate hydrophilicity. The compounds within a favorable log P value range were found to have potent in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Compounds 3a and 4h were superior to linezolid in both in vitro and in vivo potency and were considered to be hopeful compounds. We also discuss the pharmacokinetic properties of several compounds in mice.