Studies on orally active cephalosporin esters. VI. Synthesis and antimicrobial activity of 3-(3-isoxazolyl)oxymethylcephalosporin derivatives.
The synthesis and biological activities of a series of 3-(isoxazol-3-yl)oxymethyl cephalosporins are described. 7-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3- [(isoxazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid (7a) showed potent activity against both Gram-positive and Gram-negative bacteria including some beta-lactamase producing species. Its pivaloyloxymethyl ester provided a good urinary recovery after oral administration to mice.
Nakayama
E
E
Sankyo Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Watanabe
K
K
Miyauchi
M
M
Fujimoto
K
K
Ide
J
J
D001419:Bacteria / Q000187:drug effects*; D002511:Cephalosporins / Q000737:chemistry* / Q000494:pharmacology; D004952:Esters; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D002511:Cephalosporins; D004952:Esters