Studies on beta-lactam antibiotics. XII. Synthesis and activity of new 3-ethynylcephalosporin.
The synthesis of the orally absorbed 3-ethynylcephalosporin is described. In addition, the structure-activity relationships and oral absorption in rats of 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2- carboxymethoxyiminoacetamido]cephalosporins having various aliphatic hydrocarbon groups at the 3-position are discussed. Of these cephalosporins, 3-ethynyl-cephalosporin exhibited better activity against Staphylococcus aureus than the other cephalosporins and showed moderate oral absorption in rats.
K
K
Kawabata
T
T
Masugi
T
T
Takaya
D000042:Absorption; D000284:Administration, Oral; D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D002511:Cephalosporins; C048656:3-ethynylcephalosporin