99735-41-8

Upstream product

• 110-85-0 piperazine 
• 98417-05-1 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(p-tolylsulfonyl)-1,8-naphthyridine-3-carboxylic acid 
• 100361-18-0 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid 
• 96568-24-0 2-chloro-5-fluoro-6-(p-tolylthio)nicotinonitrile 
• 96568-25-1 2,5-difluoro-6-(p-tolylthio)nicotinonitrile 
• 82671-03-2 ethyl 2,6-dichloro-5-fluoropyridine-3-carboxylate 
• 114171-57-2 ethyl 2-chloro-5-fluoro-6-(p-tolylthio)nicotinate 
• 96568-26-2 ethyl 2,5-difluoro-6-(p-tolylthio)nicotinate 
• 82671-02-1 2,6-dichloro-5-fluoro-pyridine-3-carbonitrile 
• 76731-85-6 β-cyclopropylaminopropionic acid ethyl ester 
• 96568-06-8 3-cyclopropylamino-2-(2,6-dichloro-5-fluoropyridine-3-carbonyl) acrylate 
• 96568-05-7 2,6-dichloro-α-(ethoxymethylene)-5-fluoro-β-oxo-3-pyridinepropanoic acid ethyl ester 
• 96568-07-9 ethyl-7-chloro-6-fluoro-1-cyclopropyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate 
• 96568-27-3 ethyl 2-amino-5-fluoro-6-(p-tolylthio)nicotinate 

Relevant academic research and scientific papers

NOVEL METHOD OF SYNTHESIS OF FLUOROQUINOLONES

The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.

Naphthyridine antibacterial agents

Novel naphthyridine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.

6,7-disubstituted 1-cycloproply-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids

New 6,7-disubstituted-1-cyclopropyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxy lic acids of the formula (I) STR1 in which X represents halogen or nitro and A represents STR2 wherein R1, R2, R3 and R4 are defined hereinbelow are disclosed as well as their usefulness as antibacterial agents.

Fluoronaphthyridines and Quinolones as Antibacterial Agents. 1. Synthesis and Structure-Activity Relationships of New 1-Substituted Derivatives

A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated.These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position.As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin (1) or ciprofloxacin (10).Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.

4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivative as antibacterial agents

Novel naphthyridine-, quinoline- and benzoxazinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

Antibacterial agents

Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

Quinolone Antibacterial Agents. Synthesis and Structure-Activity Relationships of 8-Substituted Quinoline-3-carboxylic Acids and 1,8-Naphthyridine-3-carboxylic Acids

A series of 7,8-disubstituted 1-cyclopropyl-6-fluoroquinoline-3-carboxylic acids, 7-substituted 1-cyclopropyl-6-fluoro-1,8-naphthyridine-3-carboxylic acids, and 10-substituted 9-fluoropyridobenzoxazine-6-carboxylic acids has been prepared and evaluated for antibacterial activity.The side chains examined at the 7-position (benzoxazine 10-position) included piperazinyl (g), 3-aminopyrrolidinyl (a), 3-(aminomethyl)pyrrolidinyl (b), and alkylated 3-(aminomethyl)pyrrolidinyl (c-f).Variations ta C-8 of the quinolone ring system included hydrogen, nitro, amino, fluorine and chlorine.The relative enhancement of in vitro activities by the side chains on the 8-hydrogen quinolone and 1,8-naphthyridine against Gram-negative organisms was a > b > g > c-f.The activity imparted to the substituted quinolone nucleus by the 8-substituent was in the order F > Cl > naphthyridine > H > benzoxazine > NH2 > NO2.These trends were retained in vivo.

Antibacterial agents

Novel naphthyridine-, quinoline- and benzoxazine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

1-cyclopropyl-6,7-dihalo-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid and their esters, useful as intermediates for preparing the 7-amine substituted naphthyridines

1-cyclopropyl-6,7-dihalo-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids and their esters, which are useful as intermediates for the preparation of compounds which are useful as anti-bacterial agents.