Studies on orally active cephalosporins. II. Synthesis and structure-activity relations of new ((E) or (Z) 3-substituted carbamoyloxy)-1-propenyl cephalosporins.
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- NEGI SHIGETO
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- SASHO MANABU
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- YAMANAKA MOTOSUKE
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- SUGIYAMA ISAO
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- KOMATSU YUKI
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- TSURUOKA AKIHIKO
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- KAMADA ATSUSHI
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- TSUKADA ITARU
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- HIRUMA RYOICHI
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- KATSU KANEMASA
- Tsukuba Research Laboratories, Eisai Co., Ltd.
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- MACHIDA YOSHIMASA
- Tsukuba Research Laboratories, Eisai Co., Ltd.
書誌事項
- タイトル別名
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- II. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONS OF NEW [(<i>E</i>) OR (<i>Z</i>) 3-SUBSTITUTED CARBAMOYLOXY]-1-PROPENYL CEPHALOSPORINS
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説明
In an effort to find a new oral cephalosporin with well-balanced antibacterial spectrum, good oral absorbability and long plasma half-life, a series of oxyimino aminothiazolyl 3-[(E)- or (Z)-N-substituted carbamoyloxy]propenyl cephems was synthesized and evaluated for antibacterial activity and oral absorbability. The substituents of the carbamoyloxy group affected their in vitro activity and bioavailability after oral administration of their pivaloyloxymethyl esters at the C-4 position. The compound possessing an N, N-dimethylcarbamoyloxy moiety at the C-3 position showed good oral absorption and well-balanced antibacterial activity. In this report, the structure-activity relationships and the structure-oral absorbability relationships of 3-(N-substituted carbamoyloxy)-propenyl cephems are described.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 47 (12), 1526-1540, 1994
公益財団法人 日本感染症医薬品協会