SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF TITUTED-2-AMINOPROPIONAMIDO]-3-VINYLCEPHALOSPORINS AND RELATED-COMPOUNDS

A series of new 7 a-[3-(un)substituted-alanyl]-3-vinylcephalosporins a nd some related compounds, 4a-l is described. They incorporate residue s of proteinogenic L-alpha-aminocarboxylic acids, their antimetabolite s and enantiomers as well as a dipeptide in the 7 beta-acylamido side chain. The acylation of diphenyl-methyl 7-amino-3-vinyl-3-cephem-4-car boxylate (2: R(2)=DPM) with various protected alpha-aminocarboxylic ac ids 1a-k and the dipeptide 1l is carried out using TBTU as coupling re agent. The compounds, except 4f, are active in vitro against S. aureus and S. lutea, but only 4a, 4k, and 4l inhibit some of the Gram-negati ve strains.