Semisynthetic β-Lactam Antibiotics. IX. Synthesis and Antibacterial Activity of 7-[2-(2-Aminothiazol-4-yl)-2-sulfoacetamido]-cephalosporanic Acid and Its Derivatives
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概要
- 論文の詳細を見る
Novel 2-(2-aminothiazol-4-yl)-2-sulfoacetyl cephalosporins (10a-c) were synthesized by two routes : A, acylation of 7-aminocephalosporanic acid (8a) or its analogs (8b, c) with an active derivative of 2-(2-aminothiazol-4-yl)-2-sulfoacetic acid, and B, side chain sulfonation of γ-chloroacetoacetyl cephalosporins (13a, b) with SO_3-dioxane and subsequent thiazole ring formation by treatment with thiourea. The cephalosporin with 4-carbamoylpyridiniomethyl at the 3-position (10c) showed a potent antipseudomonal activity but had poor activity against other gram-negative bacteria, while the cephalosporin with 1-methyltetrazol-5-ylthiomethyl at the 3-position (10b) showed a broad spectrum but caused no inhibition of Pseudomonas aeruginosa.
- 公益社団法人日本薬学会の論文
- 1983-02-25
著者
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南 功
Central Research Division Takeda Chemical Industries Ltd.
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野村 容朗
Central Research Division, Takeda Chemical Ind., Ltd.,
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近藤 正煕
Central Research Division Takeda Chemical Industries Ltd.
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野村 容朗
Research and Development Division, Eisai Company, Ltd.,
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秋元 浩
Central Research Division, Takeda Chemical Industries, Ltd.
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野村 容朗
Research And Development Division Eisai Company Ltd.
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Nomura Hiroaki
Research And Development Division Eisai Company Ltd.
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秋元 浩
武田薬品工業(株)
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秋元 浩
武田薬品工業
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秋元 浩
武田薬品工業(株)化学研究所
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