Antibacterial and beta-lactamase inhibitor beta-lactam cpds. - which are methyl-substd. 3,7-di:oxo-1-aza-bi:cyclo-(3,2,0)-heptan-2-carboxylic acid derivs.

摘要

New beta-lactam cpds. are des-thia-penicillonic acid derivs. of formula (I) and their physiologically acceptable salts. R1, R2 and R3 are H or Me, at least one being Me; R4 is H, Cl, Br or OH; R5 is H, 1-4C alkyl, benzyl, nitrobenzyl, methoxybenzyl or a readily hydrolysable residue; and R6 is H, 1-6C alkyl, 1-4C hydroxyalkyl, benzyl or alpha-hydroxybenzyl. (I) are well tolerated cpds. with broad spectrum in vitro and in vivo activity against pathogenic microorganisms such as gram- positive and gram-negative bacteria (including strains resistant to usual cephalosporin and penicillin antibiotics). (I) also have beta-lactamase inhibiting activity against beta-lactamases from gram-positive and gram-negative microorganisms. In addition, (I) are useful as intermediates for other pharmaceuticals (e.g. thienamycin derivs. with beta-lactamase inhibiting and antibacterial activity).