245554-83-0

Upstream product

• 1196-57-2 quinoxalin-2⁽¹⁾-one 
• 52798-46-6 3-Cyanophenylglyoxylsaeuremethylester 
• 95-54-5 1,2-diamino-benzene 
• 1029649-48-6 tert-butyl (2-isocyanophenyl)carbamate 
• 1360877-55-9 2-(3-cyanophenyl)-2-oxoacetic acid 
• 245554-81-8 3-(3-bromophenyl)-3,4-dihydro-1H-quinoxalin-2-one 
• 544-92-3 copper(I) cyanide 
• 245554-82-9 3-(3-bromophenyl)-1H-quinoxalin-2-one 

Downstream Products

• 245554-84-1 3-[4-(5-bromopentyl)-3-oxo-3,4-dihydroquinoxalin-2-yl]benzonitrile 
• 745018-47-7 3-{4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxalin-2-yl}benzonitrile 

Relevant academic research and scientific papers

High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators

We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC50 of ～200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here, structure-activity studies were done on 36 synthesized phenylquinoxalinone analogs to identify compounds with improved potency and altered metabolic stability. Synthesis of the phenylquinoxalinone core was generally accomplished by condensation of 1,2-phenylenediamines with substituted phenyloxoacetates. Structure-activity studies established, among other features, the privileged nature of a properly positioned nitro moiety on the 3-aryl group. Synthesized analogs showed improved CFTR activation potency compared to 4 with EC50 down to 21 nM and with greater metabolic stability. CFTR activators have potential therapeutic indications in constipation, dry eye, cholestatic liver diseases, and inflammatory lung disorders.

Facile One-Pot Synthesis of Benzimidazole and Quinoxalin-2(1 H)-one Scaffolds via Two-Component Coupling Reaction, Deprotection, and Intermolecular Cyclization

Two scaffolds, namely benzimidazole and quinoxalin-2(1H)-one, were synthesized by treating 2-(N-Boc-amino)phenylisocyanide (Boc: tert-butoxycarbonyl) with carboxylic acids and glyoxylic acids, respectively. The target compounds were generated directly aft

Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa

Factor Xa (FXa) has materialized as a key enzyme for the intervention of the blood coagulation cascade and for the development of new antithrombotic agents. FXa is the lone enzyme responsible for the production of thrombin and therefore is an attractive t

Quinoxalinones as serine protease inhibitors such as factor XA and thrombin

This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.