Abstract: The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.

Abstract: A heteroanellated phenylglycine-.beta.-lactam antibiotic of the formula ##STR1## in which R.sup.

Abstract: Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.

Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.

Abstract: New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom,R.sub.3 denotes a hydrogen atom,R.sub.4 denotes a hydrogen atom, an optionally substituted naphthyl radical or a radical of the general formula ##STR2## and the remaining variables can be various organic radicals.

Abstract: Anti-bacterially active penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom or optionally substituted alkoxy group,R.sub.3 denotes a hydrogen atom, COR.sub.4, SO.sub.2 -alkyl, SO.sub.2 -aryl or an optionally substituted alkyl group, but R.sub.2 and R.sub.3 do not simultaneously denote hydrogen atoms, andR.sub.4 denotes a hydrogen atom or any of many possible organic radicals.The compounds are also inhibitors of .beta.-lactamases so they can be used in conjunction with .beta.-lactamase-susceptible antibiotics. They are useful in fighting bacterial infection, in promoting animal growth and in preserving various materials.

Abstract: 6-[.alpha.-(Imidazolidin-2-on-1-ylcarbonylamino)-substutited acetamido]penicillanic acids, and the correspondingly 7-substituted ceph-3-em-4-carboxylic acids, characterized by the presence of a methyleneamino or substituted methyleneamino group on the 3-nitrogen atom of the imidazolidine ring are antibacterial agents. The compounds, of which 6-[.alpha.-(3-benzaliminoimidazolidin-2-on-1-ylcarbonylamino)cyclohe xa-1,4-dien-1-ylacetamido]penicillanic acid and 7-[.alpha.-(3-furylideneaminoimidazolidin-2-on-1-ylcarbonylamino)phenylace tamido]-3-(3-methylthiadiazol-5-ylthiomethyl)ceph-3-em-4-carboxylic acid are typical examples, are prepared through acylation of an 6-[.alpha.-(amino)substituted acetamido]penicillanic acid or the corresponding 7-[.alpha.-(amino)substituted acetamido]ceph-3-em-4-carboxylic acid with a reactive nucleofugic derivative of a 3-methyleneaminoimidazolidin-2-on-1-carboxylic acid.

Abstract: Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

Abstract: Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is -CO- or -SO.sub.2 -, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is -CO-,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

Abstract: Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, whereinA is hydrogen; unsubstituted or substituted alkyl; aryl; or R.sub.1 --X--, whereinX is --CO-- or --SO.sub.2 --, andR.sub.1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl;Or whenX is --CO--,R.sub.1 can also be alkoxy;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety ##STR2## E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

Abstract: .beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC* constitutes a center of chirality; are produced which exhibit antibiotic activity.

Abstract: .beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC constitutes a center of chirality;Are produced which exhibit antibiotic activity.

Abstract: .beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or cyclohexa-1,4-dien-1-yl;R is a moiety of the formula ##STR2## wherein E is hydrogen, --OH or --O--CO--CH.sub.3 ; andC* constitutes a center of chirality;Are produced which exhibit antibiotic activity.

Abstract: 6-[.alpha.-(Imidazolidin-2-on-1-carbonylamido)acetamido]-penicillanic acids substituted in the 3-position of the imidazolidinone ring with phenyl or a substituted phenyl group and on the .alpha.-carbon atom of the acetamido bridge with a phenyl, thienyl, cyclohexenyl or cyclohexadienyl group, and their salts, are antibacterial agents. The compounds, of which .alpha.-(3-phenylimidazolidin-2-on-1-ylcarbonylamino)benzylpenicillin is a representative example, are prepared by acylation of the corresponding 6-(.alpha.-aminoacetamido)penicillanic acid or a derivative thereof.

Abstract: 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.

Abstract: Penicillins of the formula ##STR1## or pharmaceutically acceptable non-toxic salts thereof, wherein C* is a carbon atom constituting a center of chirality;A is a moiety of the formula ##STR2## wherein X is ##STR3## Y is ##STR4## WHEREIN Aryl is an aryl moiety; Z is ##STR5## Q.sub.1 is ##STR6## Q.sub.2 is ##STR7## R is straight-chain or branched alkyl of 1 to 5 carbon atoms; R.sub.1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms, vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H.sub.2 N--, R--NH--, (R).sub.2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S--V--, N=C--V--, R--O--CO--V--, H.sub.2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO.sub.2 --NH--, (R).sub.2 N--CO--V--, wherein R is as above defined, ##STR8## provided that when X is --SO.sub.2 --, R.sub.

Abstract: A compound of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR.sub.1 is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;A is a moiety of the formula: ##EQU1## wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;B is a moiety of the formula: ##SPC2##WhereinR.sub.8, r.sub.9 and R.sub.

Abstract: A compound of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR.sub.1 is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;A is a moiety of the formula: ##EQU1## wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen, straight or branched chain alkyl of 1 to 5 carbon atoms, monoaralkyl of up to 8 carbon atoms, monoaryl, substituted monoaryl, or thienyl;B is a moiety of the formula: ##SPC2##WhereinR.sub.8, r.sub.9 and R.sub.

Abstract: Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamido or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.

Abstract: 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.