Lipidic peptides. IV. Penicillin and cephalosporin amide conjugates with lipidic amino acids and their oligomers

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A series lipidic amide conjugates ( 2b, c, 3b, c, 4b-d, 5b and c) of β-lactam antibiotics were synthesised using mixed anhydride methods to couple the Boc-protected lipidic amino acids ( 1a and b) and oligomer ( 1c) to a variety of penicillins and cephalosporins. Conjugates ( 2b, c, 3b, 4b-d and 5b) showed weak to moderate activity in vitro and were only weakly active in vivo against the non-β-lactamase producing stain S. aureus 663E.