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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  • 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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Description

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.

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Details 詳細情報について

  • CRID
    1390282679125084032
  • NII Article ID
    130003502687
  • DOI
    10.7164/antibiotics.47.1526
  • COI
    1:CAS:528:DyaK2MXivVCqtb0%3D
  • ISSN
    18811469
    00218820
  • PubMed
    7844046
  • Text Lang
    en
  • Article Type
    journal article
  • Data Source
    • JaLC
    • Crossref
    • PubMed
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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