Studies on Prodrugs of Cephalosporins. I. Synthesis and Biological Properties of Glycyloxybenzoyloxymethyl and Glycylaminobenzoyloxymethyl Esters of 7β-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-methyl-3-cephem-4-carboxylic Acid

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p-Glycyloxy-, o-glycylamino- and p-glycylaminobenzoyloxymethyl esters of 7β-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-methyl-3-cephem-4-carboxylic acid (1) were synthesized as prodrugs designed to improve the oral absorption of the parent cephalosporin. The esters were found to possess the desired factors for an orally active prodrug, that is, appropriate solubility, lipophilicity and lability. As predicted from these factors, the esters when administered orally to mice were well absorbed from the gastrointestinal tract and gave high blood levels of the parent compound (1).
公益社団法人日本薬学会の論文
1984-02-25