FK482(Cefdinir)に関する研究(第4報)7β-[(Z)-2-(2-Aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-substituted Cephalosporin誘導体の合成並びに構造活性相関
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The synthesis of 7β-[(Z)-2-(aminothiazol-4-yl)-2-hydroxyiminoacetamido] cephalosporins (Ia-i) modified at the C-3 position of a cephem nucleus and the effect of the C-3 substituents on the antibacterial activity and oral absorbability are discussed. The cephems (Ie, h and i) having a C-3 substituent such as 1-propenyl, ethylthio and vinylthio group as well as FK482 (cefdinir) exhibited excellent antibacterial activities against both gram-positive and gram-negative bacteria. However, those compounds showed poor absorption rate after oral administration in rats. It is concluded that the vinyl moiety at the 3-position is necessary to display fairly oral absorptivity in a series of 7β-[(Z)-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido] cephems.
- 公益社団法人日本薬学会の論文
- 1990-12-25
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- FK482(Cefdinir)に関する研究(第4報)7β-[(Z)-2-(2-Aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-substituted Cephalosporin誘導体の合成並びに構造活性相関
- FK482(Cefdinir)に関する研究(第3報)7β-[(Z)-2-Aryl-2-hydroxyiminoacetamido]-3-vinyl-3-cephem-4-carboxylic Acid誘導体の合成並びに構造活性相関
- FK482に関する研究(第2報)7β-[(Z)-2-(2-Aminothiazol-4-yl)-2-substituted acetamido]-3-vinyl-3-cephem-4-carboxylic Acid誘導体の合成並びに構造活性相関