1,3-Dithiol-2-on-4-yl cephalosporins - with broad-spectrum antibacterial activity

摘要

Cephalosporin derivs. of formula (I) and their salts are new (where R1 is H, acetoxy, azido, 1,3,4-thiadiazol-2-ylthio (opt. substd. by 1-4C alkyl, alkoxy, alkylthio, alkylsulphonyl, NH2 or acetylamino), 1,2,3,4-tetrazol-5-ylthio, (opt. 1-substd. by 1-4C alkyl, hydroxyalkyl, Ph or hydroxyphenyl or 2-substd. by 1-4C alkyl or hydroxyalkyl), 1,2,4-triazol-3-ylthio, 4-methyl-1,3-thiazol-2-ylthio, 3-methyl-1,2,4-thiadiazol-5-ylthio or 1,2,3-thiadiazol-4-ylcarbonylthio; R2 is COOH or COO-CHR3-O-COR4, where R3 is H or 1-4C alkyl and R4 is 1-4C alkyl or cyclohexyl and the -CHR3OCOR4 gp. is enzymatically removable; or R1 is pyridinio and R2 is COO-). (I) are antibacterial agents active against Gram positive and negative bacteria; e.g. they are active against Staph. aureus Smith at concns. of 0.001-20 mu g/cm3 against Staph. aureus MB9 at 0.001-20 mu g/cm2; against E. coli (Monod) at 0.1-60 mu g/cm2 and against Klebsiella pneumoniae at 0.5-150 mu g/cm2.