Structure-activity relationship (SBR) studies on oxazolidinone antibacterial agents. 2. Relationship between lipophilicity and antibacterial activity in 5-thiocarbonyl oxazolidinones

被引：52

作者：

Tokuyama, R ^{[1
]}

Takahashi, Y ^{[1
]}

Tomita, Y ^{[1
]}

Tsubouchi, M ^{[1
]}

Yoshida, T ^{[1
]}

Iwasaki, N ^{[1
]}

Kado, N ^{[1
]}

Okezaki, E ^{[1
]}

Nagata, O ^{[1
]}

机构：

[1] Hokuriku Seiyaku Co Ltd, Div Res & Dev, Katsuyama, Fukui 9118555, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2001年 / 49卷 / 04期

关键词：

oxazolidinone; antibacterial activity; structure-activity relationship; 5-thiourea oxazolidinone; 5-dithiocarbamate oxazolidinone;

D O I：

10.1248/cpb.49.353

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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).

引用

页码：353 / 360

页数：8

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