Structure-Activity Relationship (SAR) Studies on Oxazolidinone Antibacterial Agents. 2. Relationship between Lipophilicity and Antibacterial Activity in 5-Thiocarbonyl Oxazolidinones.
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- TOKUYAMA Ryukou
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- TAKAHASHI Yoshiei
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- TOMITA Yayoi
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- TSUBOUCHI Masatoshi
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- YOSHIDA Toshihiko
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- IWASAKI Nobuhiko
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- KADO Noriyuki
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- OKEZAKI Eiichi
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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- NAGATA Osamu
- Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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抄録
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).
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 49 (4), 353-360, 2001
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204163208832
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- NII論文ID
- 110003615903
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD3MXisFamtbw%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 5726078
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- PubMed
- 11310657
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可