Structure-Activity Relationship (SAR) Studies on Oxazolidinone Antibacterial Agents. 3. Synthesis and Evaluation of 5-Thiocarbamate 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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- 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
A series of 5-thiocarbamate oxazolidinones was prepared and tested for in vitro and in vivo antibacterial activities. The results of in vitro antibacterial activity indicated that the 5-thiocarbamate group was a suitable substituent for the activity by the 5-moderate hydrophilicity. The compounds within a favorable log P value range were found to have potent in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Compounds 3a and 4h were superior to linezolid in both in vitro and in vivo potency and were considered to be hopeful compounds. We also discuss the pharmacokinetic properties of several compounds in mice.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 49 (4), 361-367, 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
- 1390001204163210624
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- NII論文ID
- 110003615904
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD3MXisFamtb0%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 5726088
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- PubMed
- 11310658
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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