Orally absorbable D-forphenicinol-cephalosporins.
The synthesis and biological evaluation of D-forphenicinol-cephalosporins are described. 7-Amino-3-(substituted)-3-cephem-4-carboxylic acid esters were coupled with N-tert-butoxy-carbonyl-D-forphenicinol derivatives. Most of cephalosporin analogs in this series had good antibacterial activities and were well absorbed from the gastrointestinal tract in mice. Among them, 7-(mono-O-methyl-D-forphenicinol)-3-propenyl analog showed the most significant result in biological evaluations.
Koyama
Y
Y
Institute of Microbial Chemistry, Tokyo, Japan.
Huang
S P
SP
Ikeda
D
D
Hamada
M
M
Kondo
S
S
Takeuchi
T
T
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002511:Cephalosporins / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D005998:Glycine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D007408:Intestinal Absorption; D008297:Male; D051379:Mice; D015394:Molecular Structure; D013203:Staphylococcal Infections / Q000188:drug therapy
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; C035946:forphenicinol; D005998:Glycine