98105-65-8

Upstream product

• 371-40-4 4-fluoroaniline 
• 1117-37-9 ethyl (E)-3-(dimethylamino)acrylate 
• 86483-51-4 ethyl 2,4-dichloro-5-fluoro-benzoyl-acetate 
• 704-10-9 2,4-dichloro-5-fluoroacetophenone 
• 86393-34-2 2,4-dichloro-5-fluorobenzoyl chloride 

Downstream Products

• 98106-33-3 7-(4-Dimethylamino-piperidin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-46-8 1-(p-fluorophenyl)-6-fluoro-7-(4-butyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid 
• 98106-47-9 7-[1,4]Diazepan-1-yl-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98105-99-8 sarafloxacin 
• 98106-40-2 6-Fluoro-1-(4-fluoro-phenyl)-7-(3-methylamino-pyrrolidin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid; hydrochloride 
• 98106-39-9 1-(p-fluorophenyl)-6-fluoro-7-(3-amino-1-pyrrolidinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride 
• 98106-44-6 6-Fluoro-1-(4-fluoro-phenyl)-4-oxo-7-(4-propionyl-piperazin-1-yl)-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-38-8 7-[3-(Acetyl-methyl-amino)-pyrrolidin-1-yl]-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-00-4 7-(4-Ethoxycarbonyl-piperazin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-43-5 7-(4-Acetyl-piperazin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-42-4 7-(3-Acetylamino-pyrrolidin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-36-6 6-Fluoro-1-(4-fluoro-phenyl)-7-(4-methyl-3-oxo-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-45-7 6-Fluoro-1-(4-fluoro-phenyl)-4-oxo-7-(3-oxo-piperazin-1-yl)-1,4-dihydro-quinoline-3-carboxylic acid 
• 98106-41-3 7-(3-Dimethylamino-pyrrolidin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 

Relevant academic research and scientific papers

Enaminone amides as novel orally active GABAA receptor modulators

A series of enaminone esters and amides have been developed as potent allosteric modulators of γ-aminobutyric acidA (GABA A) receptors. The compounds bind to a novel modulatory site that is independent of the benzodiazepine (BZ), isosteric GABA, and neuroactive steroid binding sites. Structure-activity relationship (SAR) studies resulted in the synthesis of the c-Bu amide 16h with an in vitro potency of 7 nM based on inhibition of [35S]TBPS binding. The activity of the enaminones as positive allosteric modulators was confirmed with electrophysiological measurements in oocytes expressing α1β2γ 2L GABAA receptors. The i-Pr, s-Bu, c-Pr, and c-Bu amides (16e-h) were orally active in mice with profound central nervous system depressant effects. The i-Pr amide 16e was an orally active anxiolytic in the mouse light-dark paradigm.

Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents

A series of novel arylfluoroquinolones has been prepared.These derivatives are characterized by having a fluorine atom at the 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.Structure-activity relationship (SAR) studies indicate that the in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or p-hydroxyphenyl and the 7-substituent is either 1-piperazinyl, 4-methyl-1-piperazinyl, or 3-amino-1-pyrrolidinyl.The electronic and spatial properties of the 1-substituent, as well as the steric bulk, play important roles in the antimicrobial potency in this class of antibacterials.As a result of this study, compounds 45 and 41 were found to possess excellent in vitro potency and in vivo efficacy.