CP6679, a new injectable cephalosporin. Part 1: synthesis and structure-activity relationships.
A series of cephalosporins bearing a 5,5-fused ring system, an (imidazo[5,1-b]thiazolium-6-yl)methyl group, at the C-3 position were synthesized and evaluated for in vitro antibacterial activities. CP6679 (1s) and its analogues showed potent antibacterial activities against gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa. They were also highly active against methicillin-resistant Staphylococcus aureus (MRSA). CP6679 (1s) showed more potent antibacterial activity than ceftazidime (CAZ) or cefpirome (CPR) against Pseudomonas aeruginosa and MRSA.
Masakitsushima
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
Iwamatsu
K
K
Umemura
E
E
Kudo
T
T
Sato
Y
Y
Shiokawa
S
S
Takizawa
H
H
Kano
Y
Y
Kobayashi
K
K
Ida
T
T
Tamura
A
A
Atsumi
K
K
D002442:Ceftazidime / Q000494:pharmacology; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D007267:Injections; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D000097572:Cefpirome
D002442:Ceftazidime; D002511:Cephalosporins; D000097572:Cefpirome; C422850:CP 6679