ES368248A1 - New penicillins - Google Patents

Abstract

Novel carboxyl- or sulphonyl-ureido penicillins of Formula (I) and their non-toxic salts, wherein R 1 is a carboxylic or sulphonic acid acyl radical having up to 26 carbon atoms and R 2 and R 3 are the same or different and are hydrogen, alkyl which may be substituted or interrupted by hetero atoms, or optionally substituted cycloaliphatic, araliphatic, aromatic or heterocyclic radicals, or together form a cycloaliphatic or heterocyclic ring with 3 to 7 ring members which ring may be substituted or fused to other rings, are prepared by reacting a compound of Formula (II) wherein the amino and/or carboxyl groups may be protected with silyl groups, with an acyl isocyanate (V) or an N-acylcarbamic acid derivative (VI) or (VII) wherein R 1 is as above X is halogen, -SO 3 Na, -SO 3 K, -SO 3 NH 4 , A is -O- or -S- and R 7 is an alkyl, aralkyl or cycloaliphatic radical which may be substituted or interrupted by hetero atoms, or an optionally substituted aryl or heterocyclic radical. Pharmaceutical compositions having antibiotic activity against gram-positive and gramnegative bacteria comprise a penicillin of Formula I as defined above or a non-toxic salt thereof in admixture with a pharmaceutical diluent or carrier, or in unit dosage form with or without such a diluent or carrier.