Cephalosporin antibiotics. II. Synthesis and biological properties of CS-461 and related compounds.
The synthesis, structure-activity relationships, and biological properties of 3-thiazoliomethyl cephalosporins are described. 7-[2-(2-Aminothiazol-4-yl)-(Z)-2- methoxyiminoacetamido]-3-[5-(2-hydroxyethyl)-4-methylthiazoliomethyl+ ++]-3- cephem-4-carboxylate sulfate (CS-461) showed potent antibacterial activity against a wide variety of bacteria both in vitro and in vivo. Furthermore, CS-461 exhibited significantly low acute toxicity in mice.
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
E
E
Nakayama
K
K
Watanabe
M
M
Miyauchi
K
K
Fujimoto
S
S
Muramatsu
H
H
Yasuda
M
M
Fukami
J
J
Ide
D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D002511:Cephalosporins; C071014:CS 461