摘要:
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.
摘要:
New penicillin derivatives, or esters or salts thereof, of the formula ##STR1## in which R is H or alkoxy,B is a heterocyclic radical,A is an ethylene, trimethylene or o-phenylene radical,D is --co-- or a direct bond, andZ is a hydrogen atom, an optionally substituted alkyl or alkenyl group, an optionally substituted cycloalkyl, cycloalkenyl or cycloalkadienyl group, an optionally substituted aryl group, an optionally substituted hetercyclyl group or an acyl radical.
摘要:
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)cyclohexa-1,4-dien-1-ylacetamido]penicillanic acid and 7-[.alpha.-(3-furylideneaminoimidazolidin-2-on-1-ylcarbonylamino)phenylacetamido]-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.
摘要:
Novel cephalosporins of the formula ##STR1## in which R.sup.1 is an aliphatic or cycloaliphatic hydrocarbyl radical of up to 6 carbon atoms which is optionally substituted by a carboxyl group, ##STR2## R.sup.2 and R.sup.3 each independently is an optionally substituted aliphatic or cycloaliphatic hydrocarbyl radical of up to 6 carbon atoms, but is not unsubstituted methyl,or pharmaceutically acceptable salts thereof, are effective antibacterially and promote the growth of animals.
摘要:
Substituted 6-hydroxymethyl-carbapenem antibiotics of the formula ##STR1## in which R.sup.1 is --OR.sup.4, ##STR2## A is a direct bond, or an alkylene and/or cycloalkylene radical, R.sup.2 is a group of the formula ##STR3## an aryl or heterocyclic radical, ##STR4## R.sup.3 is a COOH radical, or salt or ester thereof.
摘要:
Antibiotically active penicillins and cephalosporins of the formula ##STR1## in which Z is hydrogen or lower alkoxy,n is 1 or 2,Y, in the form of the free acid, is ##STR2## X is --S--, --n--, --SO-- or --SO.sub.2 --, T is an organic radical, hydrogen or halogen,A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring,or non-toxic pharmaceutically tolerated salts thereof.
摘要:
Compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or an optionally substituted, straight-chain or branched alkyl or mono- or poly-unsaturated alkenyl radical with in each case up to 30 C atoms,X represents CH.sub.2, O, S or NR,whereinR denotes hydrogen or an alkyl group with up to 20 C atoms, andR.sup.2 represents hydrogen or an optionally substituted, straight-chain or branched, saturated or mono- or poly-unsaturated hydrocarbon radical with up to 30 C atoms,or pharmaceutically acceptable salts thereof, stimulate the immune system and help fight infection.
摘要:
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.
摘要:
New antibiotics of the formula ##STR1## in which X is O or N--CO--NH.sub.2,R is the radical of an aminoacid other than serine, an oligopeptide other than HyoHyoHyoSer or a derivative thereof on the free amino group, or a radical from the group comprising HyoSer, HyoHyoSer, HyoHyoHyoAla, HyoHyoHyoThr, Hyo, HyoHyo or HyoHyoHyo, andHyo is N.sup.5 -acetyl-N.sup.5 -hydroxy-L-ornithine.The intermediate wherein R is H is also new as is the tripeptide ##STR2##
摘要:
The invention relates to 3-sulphonyl-benzo-1,2,4-triazines and their 1-oxides, useful as antibacterial and antifungal agents. Also included in the invention are methods for the preparation of said benzo-1,2,4-triazine compounds, pharmaceutical compositions containing said benzo-1,2,4-triazines and methods for the use of said compounds and compositions.