Structure-Activity Relationship(SAR)Studies on Oxazolidinone Antibacterial Agents.2.^<1)> Relationship between Lipophilicity and Antibacterial Activity in 5-Thiocarbonyl Oxazolidinones
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概要
- 論文の詳細を見る
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 moleucle. 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).
- 公益社団法人日本薬学会の論文
- 2001-04-01
著者
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吉田 隆志
Department Of Pharmacognosy College Of Pharmaceutical Sciences Matsuyama University
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Nagata O
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Nagata Osamu
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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IWASAKI Nobuhiko
Research Division, Hokuriku Seiyaku Co., Ltd.
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Kado Noriyuki
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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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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OKEZAKI Eiichi
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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Yoshida T
Department Of Microbiology Hiroshima University School Of Medicine
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Tomita Y
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Okezaki E
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Tokuyama Ryukou
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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KADO Noriyuki
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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Takahashi Yoshiei
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kado Noriyuki
Research And Development Headquaters Hokuriku Seivaku Co. Ltd.
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Kado Noriyuki
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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吉田 隆志
College Of Pharmaceutical Sciences Matsuyama University
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Takahashi Y
Analytical Instruments Division Jeol Ltd.
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Nagata O
Narch
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Iwasaki N
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Tsubouchi M
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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