Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Structure-Activity Relationship (SAR) Studies on Oxazolidinone Antibacterial Agents. 1. Conversion of 5-Substituent on Oxazolidinone
Ryukou TOKUYAMA, Yoshiei TAKAHASHI, Yayoi TOMITA, Tomio SUZUKI, Toshihiko YOSHIDA, Nobuhiko IWASAKI, Noriyuki KADO, Eiichi OKEZAKI, Osamu NAGATA
Author information
Keywords: oxazolidinone, antibacterial activity, 5-substituted oxazolidinone, structure-activity relationship
JOURNAL FREE ACCESS

2001 Volume 49 Issue 4 Pages 347-352

Details
Download PDF (71K)
Download citation RIS

(compatible with EndNote, Reference Manager, ProCite, RefWorks)

BIB TEX

(compatible with BibDesk, LaTeX)

Text
How to download citation
Contact us
Abstract

A structure-activity relationship (SAR) study on 5-substituted oxazolidinones as an antibacterial agent is described. The oxazolidinones, of which 5-acetylaminomethyl moiety was converted into other functions, were prepared and evaluated for antibacterial activity. Elongation of the methylene chain (8) and conversion of the acetamido moiety into guanidino moiety (12) decreased the antibacterial activity. The replacement of carbonyl oxygen (=O) by thiocarbonyl sulfur (=S) enhanced in vitro antibacterial activity. Especially, compound 16, which had the 5-thiourea group, showed 4-8 stronger in vitro activity than linezolid. Our SAR study revealed that the antibacterial activity was greatly affected by the conversion of 5-substituent.

Content from these authors
© 2001 The Pharmaceutical Society of Japan
Next article
Favorites & Alerts

Recently viewed articles
Share this page
feedback
 Top