153163-92-9Relevant articles and documents
Novel cephalosporin derivatives possessing a bicyclic heterocycle at the 3-Position. Part I: Synthesis and biological activities of 3-(benzothiazol-2-yl)thiocephalosporin derivatives, CP0467 and related compounds
Tsushima, Masaki,Iwamatsu, Katsuyoshi,Tamura, Atsushi,Shibahara, Seiji
, p. 1009 - 1017 (2007/10/03)
A series of cephalosporin derivatives with various bicyclic heterocycles at the C-3 position was synthesized and evaluated for antibacterial activity. Among them CP0467 (3a) showed excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) (MIC90=6.25μg/mL), and extremely high affinity for the penicillin binding protein 2' of MRSA (I50=0.49μg/mL). Furthermore, 3a showed a long-acting pharmacokinetic profile in mice (AUC(∞)=482.3μg/h/mL and T(1/2)=1.9h). Copyright (C) 1998 Elsevier Science Ltd.