| 摘要 |
<p>Cephalosporins of formula (I) and their keto tautomers and salts are new. Y is H or OMe; A is phenyl, 4-hydroxyphenyl, 3,4-dihydroxyphenyl, 3-chloro-4-hydroxyphenyl, 2- or 3-thienyl, or 2- or 3-furyl; D is OCOMe, OCONH2, or SHet, where Het is 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 1,2,4-thiadiazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 4H-5,6-dioxo-1,2,4-triazin-3-yl, 4-methyl-5,6-dioxo-1,2,4-triazin-3-yl, 1-methyl, 1-vinyl, or 1-allyl-5-tetrazolyl or 1-R1-5-tetrazolyl, where R1 is 2-4C alkyl, 2,3-dihydroxypropyl or (CH2)nR'1, where n is 1-3 and R'1 is OH, NH2, NMe2, NHCOMe, CONH2, NHCONH2, SO2NH2, NHSO2NH2, NHSO2Me, CN, NHSO3H, SO2Me, SOMe, COOH or SO3H; with the proviso that D must be SHet' when Y is H, where Het' is 4H-5,6-dioxo-1,2,4-triazin-3-yl, 1-vinyl or 1-allyl-5-tetrazolyl or 1-R1-5-tetrazolyl. R is NH-Ar-Y'-R2, where Ar is p-phenylene, Y' is SO2NH, SO, or SO2, and R2 is a 5- or 6-membered heterocyclic ring, opt. substd. by Me, halogen, CN, NH2, NHMe, NMe2, alkanoylamino, alkoxycarbonylamino, OH, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, NHSO2Me, CONH2, alkanoyloxy, alkoxycarbonyl, SO2NH2, mono- or dialkylaminosulphonyl, COOH or SO3H; E is H or a protecting gp.S (I) are antibacterial agents active against Gram-positive and -negative bacteria, e.g. with MIC values of less than 0.1 mcg/ml against E. coli and K. pneumoniae and less than 10 mcg/ml against PS. aeruginosa.</p> |
