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 Original Research Article

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=6.25 μg/mL), and extremely high affinity for the penicillin binding protein 2′ of MRSA (I50=0.49 μg/mL). Furthermore, 3a showed a long-acting pharmacokinetic profile in mice (AUC∞=482.3 μg/h/mL and T1/2=1.9 h).