6-Pyrimidyl:ureido:acetamido-penicillin derivs. - used as antibacterials, feedstuff additives and preservatives

摘要

Penicillins of formula (I), their pyrimidone tautomers and their physiologically accetable salts with bases are new: In (I), A is phenyl, 4-hydroxyphenyl, 2- or 3-thienyl, cyclohexyl, cyclohex-1-enyl, cyclohexa-1,4-dienyl or 3,4-disubstd. phenyl in which the substits. are same or different Cl, OH or OMe. R is e.g. H, 1-8C aliphatic hydrocarbyl (opt. contg. 1 or 2 double bonds or a triple bond), cyclopropyl (opt. substd. by 1 or 2 Me gps. or an Et or Ph gp), 4-8C cycloalkyl (opt contg. >=1 double bond), beta-phenethyl, gamma-phenylpropyl, beta-phenylethylidene, cyclopropylmethyl, 1-cyclopropylethyl, OH, 1-8C alkoxy, 2-8c alkenyloxy, 3-6C cycloalkoxy, OPh, OCH2Ph, SH, 1-8C alkylthio, 3-6C cycloalkylthio, SPh, SCH2Ph, p-chlorobenzylthio, 1-4C alkylsulphinyl, morpholino or thiamorpholino (or its S-oxide or S,S-dioxide). (I) are broad-spectrum antibacterial agents which give high serum and tissue levels on oral or parenteral administration. They can be used in human or veterinary medicine at daily doses of 5-500 mg/kg. LD50 is >4 g/kg mouse p.p. (I) can also be used as animal feedstuff additives for promoting growth and improving fodder utilisation and as preservatives e.g. for polymers, lubricants, paints fibres, leather, paper, wood and foods.