摘要:
New .beta.-lactams of the general structure: ##STR1## wherein R represents H or an acyl moiety known from the penicillin or cephalosporin art, R' is hydrogen, loweralkoxy, loweralkoxyalkyl, loweralkyl, phenylthio or loweralkylmercapto R" is loweralkyl, the broken line represents an optional double bond, and acyloxymethyl esters thereof. All compounds are effective antibacterials.
摘要:
It has been found that dipeptides containing a 3-fluoro-D-alanine N-terminus are powerful antibacterials and produce a highly useful synergistic effect with antibiotics.
摘要:
Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having the formula ##STR1## wherein A is sulfur or oxygen; R.sup.1 is selected from the group consisting of hydroxy, protected-hydroxy, C.sub.1 -C.sub.6 -alkoxy, halo, amino, C.sub.1 -C.sub.6 -alkylamino, hydroxy-C.sub.1 -C.sub.6 -alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R.sup.2 is selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 -alkyl, or halo-C.sub.1 -C.sub.6 -alkyl; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl; and R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxyl, having utility as intermediates or having antibacterial or antineoplastic activity
摘要:
Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds whereinA is.dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要:
A process for producing racemic or optically active compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 to C.sub.6 alkyl or benzyl; and Z is amino or substituted amino. Also disclosed are intermediates useful in the process and methods for producing the intermediates.
摘要:
New 7-substituted 6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids or esters having a substituted or unsubstituted phenyl radical, an aromatic heterocyclic radical, an alkyl or cycloalkyl radical in the 1-position are antibacterial agents.
摘要:
Quinoline compounds having the formula: ##STR1## wherein R is a phenyl group or an aromatic heterocyclic group, Z is an aliphatic heterocyclic group or an amine, and R.sub.1 is hydrogen or a carboxy-protecting group. The compounds here disclosed have antibacterial properties.
摘要:
1-pyridine substituted quino-benoxazines having the formula: ##STR1## wherein X is halogen or hydrogen; R.sub.2 is a substituent; and R.sub.1 is hydrogen or a carboxy protecting group.
摘要:
Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is .dbd.CR.sup.6 --; R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; and R.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要:
Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas: ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas: ##STR2## with the assistance of a streochemically directing chiral oxazolidinone moiety having the formula: ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated add chloride, reaction with N-benzyl-N-(methoxymethyl)trimethyl-silylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.