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.
Nakayama
E
E
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Watanabe
K
K
Miyauchi
M
M
Fujimoto
K
K
Muramatsu
S
S
Yasuda
H
H
Fukami
M
M
Ide
J
J
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