7-Alpha methoxy cephalosporin cpds. - are antimicrobials prepd. from amino cephalosporanic acid and a sulphinyl carboxylic acid

摘要

7-alpha-Methoxycephalosporin derivs. of formula (I) in which the sulphinyl gp. is in the R form, and their sales and esters, are new. (where R1 = lower alkyl or alkynyl, aryl, aralkyl, heterocyclyl or heterocyclyl lower alkyl, these gps. opt. being substd. by =1 of halogens, NO2, OH, lower alkenyl, lower alkoxy, azido, amino, substd. amino, carboxy, carboxy lower alkyl, CF3, CN, NH2CONH, SH, CONH2, sulphinyl, sulphonyl, hydrazino, formyl, acetoxy, lower acylamino, lower alkylamino, lower acyl, carbonyl, thio, hydroxyamino, lower alkyl, carbonyl, thio, hydroxyamino, lower alkyl, lower hydroxy alkyl, lower alkoxymethyl, N-oxo, lower carboalkoxy or thiocarbonyl; R2 = 1-3C straight or branched, alkylene chain which may be substd. by CH3; X = H, acetoxy, quat. ammonium carbamoyloxy, lower alkoxy, lower alkylmercapto or heterocyclic mercapto, the heterocyclic mercapto gp. opt. being substd. by the same substituents as for R1; and the R form signifies an optical isomer having the same stereochemical structure as the optical isomer of The two isomers of the sulphinyl gp. of the cpd. R1-SO-R2-COOH (II), which has a positive specific rotatory power in ethanol). (I) are active against Gram positive and negative bacteria and partic. useful against choleoystitis, septicaemia and nephropyelitis.