cas 452092-31-8, 1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-hydroxy-4-oxo-3-quinolinecarboxylic Acid Ethyl Ester

Articles about 452092-31-8Total 6 be found

Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones
Conformationally constrained tetracyclic fluoroquinolones (FQs) were synthesized and profiled for their microbiological spectrum. The installation of a seven-membered ring between the pyrrolidine substituents and the C8 position on the FQ core scaffold resulted in a remarkable enhancement of microbiological potency toward both Gram-positive and Gram-negative bacteria. Focused optimization of seven-membered ring composition, stereochemistry, and amine placement led to the discovery of the two lead compounds that were selected for further progression.
Wagman, Allan S.,Cirz, Ryan,McEnroe, Glenn,Aggen, James,Linsell, Martin S.,Goldblum, Adam A.,Lopez, Sara,Gomez, Marcela,Miller, George,Simons, Lloyd J.,Belliotti, Thomas R.,Harris, Christina R.,Poel, Toni-Jo,Melnick, Michael J.,Gaston, Ricky D.,Moser, Heinz E.
p. 1687 - 1692
(2017/10/09)

Novel Antibacterial Compounds
The invention relates to novel chimeric antibiotics of formula I wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl;R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6;R3 is H or halogen;R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl;R5 is alkyl or haloalkyl; andR6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
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Page/Page column 21

(2010/09/07)

5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE ANTIBACTERIALS
The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen
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Page/Page column 38

(2008/12/05)

Aminoquinolones as GSK-3 inhibitors
Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.
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Page/Page column 81-82; 122

(2008/06/13)

NOVEL ANTIBACTERIAL COMPOUNDS
The invention relates to novel chimeric antibiotics of formula (I) Wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
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Page/Page column 55

(2010/11/25)

QUINOLONECARBOXYLIC ACID COMPOUNDS, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
This invention discloses novel quinolonecarboxylic acid derivatives, pharmaceutically acceptable salts or hydrates thereof, and their preparation methods and medical uses. The compounds in this invention show potent antibacterial activity against broad-sp
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Page/Page column 9

(2010/11/26)