Abstract:
Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases. wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group; or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.
Abstract:
Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases. wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group; or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.
Abstract:
Antimicrobial compounds having the formula (II)as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract:
Naphthyridine and quinoline compounds having the formula: wherein A is CH or N; Z is an amine having the formula: R is o , p -difluorophenyl or p -fluorophenyl; and R₁ is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity and improved solubility and pharmacokinetic properties.
Abstract:
A process for preparing substituted 7-(piperazin-1-yl)-4-oxo-1,4-dihydro-3-quinoline carboxylic acid derivative antibacterial agents by reacting a carbamate protected piperazine derivative with a 7-halo-4-oxo-1,4-dihydro-quinoline carboxylic acid derivative.
Abstract:
Naphthyridine and quinoline compounds having the formula: wherein A is CH or N; Z is an amine having the formula: R is o , p -difluorophenyl or p -fluorophenyl; and R₁ is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity and improved solubility and pharmacokinetic properties.