Alkenoyl-amido-cephalosporin(s) - for use as broad-spectrum antibiotics

摘要

Cephalosporins of formula (I): (where n = 0 or 1, R1-3 are H or 1-5C alkyl but not 4-5C alkyl when n = 1, R4 is H, opt. substd. alkyl, phthalidyl or a cation, R5 is H or 1-3C alkyl A is H, alkoxy, halogen, or CH2Y, Y is H, acyloxy, alkoxy, opt. substd. pyridinium, opt. substd. carbamoyloxy or SR6, R6 is acyl, alkyl or an opt. substd. 5- or 6-membered heterocycle opt. fused with a 5- or 6-membered aromatic ring) are novel. Cpds. (I) are antibiotics active against Gram-positive and -negative bacteria, including penicillinase-producing Staphylococci. A typical cpd. is 7-(3-butenylamino)-cephalosporanic acid. In an example, this is prepd. from 3-butenoic acid and 7-aminocephalosporanic acid.