7-Thio:acetamido 3-(1-cyanoalkyl-tetrazole-5-yl)-thiomethyl-cephem(s) - are cephalosporin antibacterials effective against Gram-positive and negative bacteria

摘要

7-Thioacetamido-3- (1-cyanoalkyl-1,2,3,4-tetrazole-5-yl) -thiomethyl -3-cephem-4-carboxylic acid derivs of formula (I), their stereo-and other isomers, salts, antibacterial metabolites and metabolic precursors of cpds. (I) are new: In (I) Z=CN,-CONH2,-CONH-NH2, -CO-NHOH, -CS-NH2, -NH-CO-C(NH)-NH2, -C(NH)-NHR, -COOR, -NH-CO-NHR or -CO-NH-CO-NHR; R=H or 1-6C alkyl; A=2-6C, unsaturated, opt. branched hydrocarbon radical; n=O, 1 or 2; T=1-4C, opt. unsaturated, opt. -branched hydrocarbon radical and X=opt. esterified carboxy. With the condition that when Z=CN,-CONH2 or -COOR then T contains >2 C atoms. (I) are used to treat infections such as respiratory tract infections, (e.g. bronchitis, bronchopneumonia, pleursy), abdominal and hepatobilary infections (e.g. choleciptitis, peritonitis), blood and cardio-vascular infections (e.g. septicemia), urinary tract infections (e.g. pyelonephritis, cystitis), gynecological and obstetrical infections (e.g. cervicitis, endometritis) and ear, nose and throat infections (e.g. otitis, sinusitis and parotiditis). They are administered orally, rectally, parenterally, topically, by inhalation and in daily doses of 1-100mg/kg, pref. parenterally in doses of 150 mg., 1-4 times daily for adults. The cpds. may be used prophylactically e.g. as 0.2-1 wt.% disinfectant solutions.