title: CP6679, a new injectable cephalosporin. Part 1: synthesis and structure-activity relationships.
abstract: 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.
authors.affiliation: Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
authors.lastname: Masakitsushima
authors.forename: K
authors.initials: K
authors.lastname: Iwamatsu
authors.forename: E
authors.initials: E
authors.lastname: Umemura
authors.forename: T
authors.initials: T
authors.lastname: Kudo
authors.forename: Y
authors.initials: Y
authors.lastname: Sato
authors.forename: S
authors.initials: S
authors.lastname: Shiokawa
authors.forename: H
authors.initials: H
authors.lastname: Takizawa
authors.forename: Y
authors.initials: Y
authors.lastname: Kano
authors.forename: K
authors.initials: K
authors.lastname: Kobayashi
authors.forename: T
authors.initials: T
authors.lastname: Ida
authors.forename: A
authors.initials: A
authors.lastname: Tamura
authors.forename: K
authors.initials: K
authors.lastname: Atsumi
mesh_terms: 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
chemical_list: D002442:Ceftazidime; D002511:Cephalosporins; D000097572:Cefpirome; C422850:CP 6679