| 摘要 |
<p>7-Beta-R1-NH 7-alpha-R2 3-SR-CH=CH- 1-oxa-ceph-3-em-4- carboxylic acid derivs. of formula (I), as the E or Z form or their mixtures, as the syn or antiform or their mixtures and their metallic salts, nitrogen-base addition salts and acid addition salts are new. In the formulae R is e.g. (1) 2-, 3- or 4-pyridyl including their N-oxides; (2) 2-pyrimidyl; (3) 6-methyl 3-pyridazinyl-1-oxide; (4) 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, substd. in position 4 by (a) 1-2C alkyl opt. substd. by alkoxy, alkylthio or formyl, (b) allyl, 2,3-dihydroxy-propyl, 1,3-dihydroxy-2- propyl or 2-formyl-2-hydroxy-ethyl, (c) 2-3C alkyl, substd. by hydroxy, carbamoyloxy, acyloxy or acylamino (the acyl gps. are opt. substd. by amino), alkylsulphonylamino ureido, alkylureido or dialkylureido; 1 are opt. substd. by formyl; 1-2C alkoxy; (10) (a) 1-alkyl-1,2,4-triazol-5-yl opt. substd. in position 3 by alkoxycarbonyl, where alkyl and alkoxy gps. are 1-2C or (b) 1-alkyl-1,3,4-triazol-5-yl; R1 is 3-amino-4-thiazolyl-C(=N -OR3)-CO-gp. (Gp. A) or R6-CH(COOH)-CO, R3 is H, alkyl, vinyl or -CR4R5-COOH; R4, R5 independently are H or alkyl or together are 2-3C alkylene; R6 is opt. para hydroxy substd. phenyl or 2- or 3-thienyl and R2 is H or methoxy. Unless specified alkyl or acyl gps. above are 1-4C, opt. branched. Antibacterials active against gram-positive and gram-negative bacteria. In vitro (I) are active at 1-15 microgram/cc against Staph.aureus Smith sensitive to penicillin G and at 0.01-1 microgram/cc against E.coli N1HJ, and in vivo against the same organisms (I) are active at 0.5-15 mg/kg s.c and 0.01-10 mg/kg s.c. respectively in mice. The s.c. LD50 in mice is 1.5-2.5 g/Kg.</p> |
