(2)-Amino-(2)-acyloxyphenyl-acetamido cephalosporins - for use as antibacterial agents

摘要

New cephalosporins of formula (I) and their esters and salts: In the formula R is H, 1-9C alkyl opt. substd. by F, Cl, Br, COOH, 1-5C alkoxy, 1-4C alkanoyloxy or 2-5C alkoxycarbonyl, or 1-10C alkoxy opt. substd. by F, Cl, Br, 1-5C alkoxy, 1-4C alkanoyloxy or 2-5C alkoxycarbonyl; R1 is H, acetoxy or S-Het; Het is 1,2,3-triazol-5-yl, 1-methyltetrazol-5-, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiazdiazol-5-yl. Cpds. (I) are broad-spectrum antibacterials, e.g. orally effective against Staph. aureus infections at a daily dose of 10-60 mg/kg. A typical cpd. is 7- D-2-amino-2-(3-propionyloxyphenyl) acetamido -3-methyl-3-cephem-4-carboxylic acid, which may be prepd. from 7- D-2-t-butyloxycarbonylamino-2-(3-hydroxyphenyl)acetamido -3-me- thyl-3-cephem-4-carboxylic acid.