643752-95-8

Usage

Organic compound

Yes

Family

Quinolinone

Contains

Fluorine atom at the 5-position of the quinolinone ring

Usage

Building block in the synthesis of pharmaceuticals and agrochemicals

Pharmacological properties

Anticonvulsant, anxiolytic

Potential treatment

Neurological disorders, cancer

Unique properties

Chemical and biological properties due to fluorination

Importance

Medicinal chemistry, drug discovery

Upstream product

• 1003944-25-9 N-(3-fluorophenyl)-3,3-bis(methyloxy)propanamide 
• 917341-52-7 (2E)-N-(3-fluorophenyl)-3-phenylprop-2-enamide 
• 611-34-7 5-Aminoquinoline 
• 2338-73-0 5-Fluor-chinolin-N-oxid 
• 372-19-0 meta-fluoroaniline 
• 394-69-4 5-fluoroquinoline 

Relevant academic research and scientific papers

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins

The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Here, we describe NI-57 (16) as new pan-BRPF chemical probe of the bromodomain (BRD) of the BRPFs. Inhibitor 16 preferentially bound the BRD of BRPF1 and BRPF2 over BRPF3, whereas binding to BRD9 was weaker. Compound 16 has excellent selectivity over nonclass IV BRD proteins. Target engagement of BRPF1B and BRPF2 with 16 was demonstrated in nanoBRET and FRAP assays. The binding of 16 to BRPF1B was rationalized through an X-ray cocrystal structure determination, which showed a flipped binding orientation when compared to previous structures. We report studies that show 16 has functional activity in cellular assays by modulation of the phenotype at low micromolar concentrations in both cancer and inflammatory models. Pharmacokinetic data for 16 was generated in mouse with single dose administration showing favorable oral bioavailability.

DERIVATIVES AND ANALOGS OF N-ETHYLQUINOLONES AND N-ETHYLAZAQUINOLONES

Bicyclic nitrogen containing compounds and their use as antibacterials.

COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS

The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.