| 摘要 |
<p>3-Thiovinyl-cephalosporin of formula (I) having syn or anit, E or Z forms and their mixtures including their acid addition, metallic and N-base addition salts are new. In (I) R is e.g. alkyl, L-2-amino-2-carboxy-ethyl; phenyl; 2-, 3- or 4-pyridyl and their (N-oxides) 2-pyrimidinyl; 3-pyridazinyl substd. in position 6 and opt. N-oxidised or tetrazolo(4,5-b)pyridazin-6-cyl; 4) 1,4-dialkyl or 1-alkyl-5,6-dioxo 1,4,5,6-tetrahydro-1, 2,4-trazin-3-yl or 2-alkyl-5,6-dioxo-1,2,5,6-dioxi-1,2,5,6-tetrahydro-1,2,4-triazin-- 3-yl; 6) Ro is H, alkyl, vinyl or cyanomethyl; R1 is H or a group-CH(R2)(OOCR3) (easily removed by enzymes) (where R2=H or alkyl and R3= alkyl or cyclohexyl. The alkyl and acyl radicals above except where specifically specified are opt-branched and contain 1-4C atoms). (I) are a antibacterials active against gram-negative and gram-positive. In vitro tests show (I) are active against penicillin G sensitive Staph aireus (Staph aureus Smith) at 0.5-15 mg/cc and against penicillin G resistant strains (Staph. aureus MB 9) at 1-30 ug/cc. They are active against E. coli Monod at 0.001-ug/cc and against Kledsiella pneumonae at 0.06-30 ug/cc. Some cpds. are active against Proteus morganii (0.01-30ug/cc) and Enterobacter aerogenes (0.1-30ug/cc)sub-cultaneous LD50 of (I) in mice is 1.5-2.5 g/kg. Admin. may be oral, rectat, parenteral or topical.</p> |
