Cephalosporins with the (E)-thiovinyl linker with pyrimidine at C-3 position exhibiting potent activities against gram-positive strains.

Cephalosporins have been used to treat many pathogens in the clinic. However, the emergence of multidrug-resistant strains of Gram-positive bacteria caused the nosocomial infection has become a major concern.1,2) Antimicrobial agents like vancomycin, quinupristin/dalfopristin (Synercid)3) and linezolid (Zyvox)4) were developed to manage infections such as complicated skin and skin structure infection and life-threatening bacteremia. The recently isolated pathogens from hospitals are likely to reduce susceptibility to those drugs.5) Therefore, urgent need of a new agent with good safety and potent efficacy against MRSA and VRE has led us to search for a new cephalosporin. Herein, we described the synthesis of cephalosporins having the (E)-thiovinyl linker with pyrimidines ring at C-3 position and aminothiazole rings at C-7 position and their antibacterial activities as well.