Synthesis and Biological Evaluation of New Aminothiazolyl Cephalosporins with Elongated Side Chains

摘要

The elongation of the chain length at 2`position of aminothiazolylacetamido group of cephalosporin antibiotics was achieved. The derivatives with elongated side chain at 2`position were successfully synthesis and their in vitro activities were evaluated. It is indicated that there is an optimum range of the chain length in order to exhibit higher biological activities. This result could open a possibility for the development of the cephalosporin antibiotics with higher activities by further variation of the substituents at other positions. The cephalosporin derivatives with a simple (relatively non-functionalized) side chain as well as with a linear extended side chain were also prepared. Low activities of these derivatives led to a conclusion that either simple (non-functionalized) change or linear elongation of the side chain does not enhance the antibacterial activities.