Orally Active Cephalosporins(第1報)7β-[2-(R)-Amino-2-phenylacetamido]-3-(1H-1,2,3-triazol-4-yl)alkylthiomethyl-3-cephem-4-carboxylic Acid及びその関連化合物の合成並びに構造活性相関

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The synthesis, antibacterial activity and oral absorbability of 7β-[2-(R)-amino-2-phenylacetamido]-3-(1H-1,2,3-triazol-4-yl) methylthiomethyl-3-cephem-4-carboxylic acid (1a) and related compounds (1b-p and 2) are described. The replacement of 1,2,3-triazole at the C-3 position of 1a with other heteroaromatics such as 1,2,4-triazole, imidazole and so on decreased its oral absorbability in mice (1b-j). The oral absorbability was also influenced by the spacer length between C-3 of cephem nucleus and C-4 of 1,2,3-triazole. The quantitative relationship between the bioavailability and the spacer length of cephalosporins (1a and 1k-p) is discussed. These results suggest that 1,2,3-triazole in the side chain at the C-3 position of cephems plays an important role in good oral absorption through its interaction with the transport system of small intestine.
公益社団法人日本薬学会の論文
1992-09-25