Orally active 2-(alkyloxycarbonyl)-2-alkylideneethyl esters of cephalosporins

J Antibiot (Tokyo). 1992 Aug;45(8):1358-64. doi: 10.7164/antibiotics.45.1358.

Abstract

2-(Alkyloxycarbonyl)-2-alkylideneethyl esters of various aminothiazole-oxyimino cephalosporins have been synthesized and studied. They are useful alternatives to the currently existing orally active esters. Among the new esters synthesized, the 3'-azidomethyl cephem ester Ro 41-3399 (7k) presented an oral bioavailability superior to the corresponding pivaloyloxymethyl ester (9) in a rat model and was selected as a candidate for further evaluation.

MeSH terms

  • Administration, Oral
  • Animals
  • Cephalosporins / administration & dosage
  • Cephalosporins / chemical synthesis
  • Cephalosporins / pharmacokinetics*
  • Esters / pharmacokinetics
  • Intestinal Absorption*
  • Mice
  • Structure-Activity Relationship

Substances

  • Cephalosporins
  • Esters