Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 3. Synthesis and evaluation of 5-thiocarbamate oxazolidinones

Chemical & Pharmaceutical Bulletin
R TokuyamaO Nagata

Abstract

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 logP 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.

References

Aug 1, 1988·Antimicrobial Agents and Chemotherapy·D C EusticeA M Slee
Jan 12, 1934·Science·C I Bliss

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Citations

Feb 3, 2007·Chemical & Pharmaceutical Bulletin·Sunil Kumar Reddy AaramadakaMagesh Vijayan
Mar 27, 2009·Photochemistry and Photobiology·Elisa FasaniAngelo Albini
Nov 28, 2009·European Journal of Medicinal Chemistry·Vandana VarshneyDevi P Sahu
Jan 3, 2006·Bioorganic & Medicinal Chemistry Letters·Braj Bhushan LohrayPrashant Kapadnis
Sep 11, 2004·Bioorganic & Medicinal Chemistry·Braj Bhushan LohrayPurvi Pandya
Oct 20, 2009·Bioorganic & Medicinal Chemistry Letters·Vandana VarshneyDevi P Sahu
Jul 17, 2007·Chemical Biology & Drug Design·Jidong LiuWeicheng Zhou
Apr 26, 2003·Bioorganic & Medicinal Chemistry·Christian HubschwerlenHans H Locher

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