CEPHALOSPORINS HAVING A HETEROCYCLIC CATECHOL IN THE C3 SIDE CHAIN II. IMPROVEMENT OF PHARMACOKINETIC PROFILE

• Published in: Journal of antibiotics Vol. 46; no. 5; pp. 850 - 857
• Main Authors: KAMACHI, HAJIME, HASEGAWA, TOSHIFUMI, KAMEI, HIDEO, IMAE, KIYOTO, OKITA, TAKAAKI, TAMAOKA, MASAMI, MURATA, SHINJI, IIMURA, SEIJI
• Format: Journal Article
• Language: English
• Published: Tokyo JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 1993; Japan Antibiotics Research Association
• Subjects: Animals; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Bacterial Infections - drug therapy; Biological and medical sciences; Ceftazidime - pharmacology; Cephalosporins - blood; Cephalosporins - chemical synthesis; Cephalosporins - pharmacokinetics; Half-Life; Medical sciences; Mice; Microbial Sensitivity Tests; Pharmacology. Drug treatments; Structure-Activity Relationship; Molecular structure; Intramuscular administration; Optimization; Synthesis; Structure activity relation; Bacteria; Heterocyclic compound; Rodentia; Bioavailability; In vitro; Infection; In vivo; Vertebrata; Antibiotic; Chemotherapy; Cephalosporin derivatives; Mammalia; Sensitivity resistance; Treatment; Mouse; Animal; Bacteriosis; Microorganism culture; Antibacterial agent; Pharmacokinetics

7-[(Z)-2-(2-Aminothiazol-4-yl)-2-methoxy-(or hydroxy)-iminoacetamido]-3-[propen-l-yl]-cephalosporins having a variety of heterocyclic catechol in 3-position of the propenyl group were synthesized. Among them, 6, 7-dihydroxyisoquinoline derivatives, 2a and 2b, showed very high and prolonged blood lev...