| 摘要 |
1465355 Heterocyclic amido-acetamido penicillanic acids BAYER AG 11 April 1974 [14 April 1973 6 Oct 1973] 16123/74 Heading C2C Novel compounds of the Formula (I) in which A is a group and X is an -SO 2 - or -CO- group; Y is a -CO-, -CS-, group (R being a straight-chain or branched alkyl radical with 1-5 carbon atoms); (G being a hydrogen atom or a straight or branched chain alkyl radical with 1-5 carbon atoms); R 1 is an alkyl radical with 1-6 carbon atoms, or an alkenyl radical with 1-6 carbon atoms, or a cycloalkyl or cycloalkenyl radical with 1-7 carbon atoms, or an optionally substituted phenyl radical, or an -NH 2 , -NHR, -NR 2 , or -NH Aryl radical, or an alkoxy* or cycloalkoxy* radical with 1-6 carbon atoms, or an aryloxy*, thienyl, pyridyl, furyl or hydrogen* radical (R being as defined above, and provided that R 1 can only have the meaning marked * when X is a -CO- group; B is a group of the formula [in which R 2 , R 3 and R 4 are identical or different radicals selected from hydrogen, halogen, R-, RO-, RS-, R.SO-, R.SO 2 -, nitro, hydroxyl, -NR 2 , -NH.CO.R or -O.CO.R groups (R being as defined above]; Z is a -CO- or -CS- group; and C* denotes a centre of chirality, which can be in either the R- or the S- configuration ; the said acetamido-penicillanic acids being either optically pure or a mixture of diastereomers resulting from C* are obtained by reacting a compound of the formula with A-Z-W (III) (in which W is halogen, azide or -N(NO)-C 1-6 alkyl) in water in the absence of an organic solvent, at a pH 1-9 and temperature 0-50‹ C., and adjusting the pH if necessary to a value in the range 1-5 to precipitate the desired acetamido-penicillanic acid. Pharmaceutical compositions having antibacterial activity comprise compounds of Formula I above in admixture with a solid or liquefied gaseous diluent, or in admixture with a liquid diluent other than a solvent of a molecular weight less than 200 except in the presence of a surface active agent. The compositions may be in forms for administration perorally, parenterally, rectally or locally. The active ingedient (I) may also be used in fodder for animals for promoting feed utilization and growth. |
