SYNTHESIS AND IN-VITRO ANTIBACTERIAL ACTIVITIES OF 3-THIAZOL-4-YL-1-CARBA-1-DETHIACEPHALOSPORINS

The synthesis and microbiological evaluation of a new series of 3-thia zol-4-yl-carba-1-dethiacephalosporins is described. Structure activity relationship was achieved by changing substitution at the 2-position of the thiazole moiety. The result was a marked variance of microbiolo gical activity in the C7 side-chain derivatives. ATMO derivatives poss ess potent activity against both Gram-positive and Gram-negative bacte ria. For example, MICs (mu g/ml) of LY215226 against representative or ganisms are as follows: S. aureus 0.25, S. pneumoniae 0.008, H. influe nzae 0.008, E. coli 0.25, K. pneumoniae 0.008, E. cloacae 0.5, S. typh i 0.25, and M. morganii 0.25.