Structure-Activity Relationship (SAR) Studies on Oxazolidinone Antibacterial Agents. 1. Conversion of 5-Substituent on Oxazolidinone.
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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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- SUZUKI Tomio
- 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
A structure-activity relationship (SAR) study on 5-substituted oxazolidinones as an antibacterial agent is described. The oxazolidinones, of which 5-acetylaminomethyl moiety was converted into other functions, were prepared and evaluated for antibacterial activity. Elongation of the methylene chain (8) and conversion of the acetamido moiety into guanidino moiety (12) decreased the antibacterial activity. The replacement of carbonyl oxygen (=O) by thiocarbonyl sulfur (=S) enhanced in vitro antibacterial activity. Especially, compound 16, which had the 5-thiourea group, showed 4-8 stronger in vitro activity than linezolid. Our SAR study revealed that the antibacterial activity was greatly affected by the conversion of 5-substituent.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 49 (4), 347-352, 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
- 1390282679139919872
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- NII論文ID
- 110003615902
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD3MXisFamtb8%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 5726063
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- PubMed
- 11310656
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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