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. 2.1) Relationship between Lipophilicity and Antibacterial Activity in 5-Thiocarbonyl Oxazolidinones
Ryukou TOKUYAMA, Yoshiei TAKAHASHI, Yayoi TOMITA, Masatoshi TSUBOUCHI, Toshihiko YOSHIDA, Nobuhiko IWASAKI, Noriyuki KADO, Eiichi OKEZAKI, Osamu NAGATA
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Keywords: oxazolidinone, antibacterial activity, structure-activity relationship, 5-thiourea oxazolidinone, 5-dithiocarbamate oxazolidinone
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2001 Volume 49 Issue 4 Pages 353-360

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Abstract

5-Thiourea and 5-dithiocarbamate oxazolidinones were synthesized as a continuation of research on 5-thiocarbonyl oxazolidinone antibacterial agents considering the hydrophobic parameters of the molecule. The structure-activity relationship (SAR) study revealed that the antibacterial activity on 5-thiocarbonyl oxazolidinones was significantly affected by the lipophilicity, especially the calculated log P value and the balance between 5-hydrophilic (or hydrophobic) substituent and hydrophobic (or hydrophilic) substituents on the benzene ring. Some of 5-thiocarbonyl oxazolidinones were found to have good in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).

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© 2001 The Pharmaceutical Society of Japan
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