1287795-35-0

Upstream product

• 1765-93-1 4-fluoroboronic acid 
• 36856-91-4 2-bromo-quinoxaline 
• 53631-18-8 2-bromo-1-(3-fluorophenyl)ethanone 
• 95-54-5 1,2-diamino-benzene 
• 455-36-7 1-(3-fluorophenyl)ethanone 
• 121247-01-6 2-(3-fluorophenyl)-2-oxoacetaldehyde 
• 768-35-4 3-fluorophenylboronic acid 

Downstream Products

• 1446862-46-9 1-methyl-3-(3-fluorophenyl)quinoxalinium iodide 
• 1287795-38-3 (R)-2-(3-fluorophenyl)-1,2,3,4-tetrahydroquinoxaline 

Relevant academic research and scientific papers

Antimicrobial agents

The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

Quinoxaline derivatives: Novel and selective butyrylcholinesterase inhibitors

Alzheimer's disease (AD) is a progressive brain disorder which occurs due to lower levels of acetylcholine (ACh) neurotransmitters, and results in a gradual decline in memory and other cognitive processes. Acetycholinesterase (AChE) and butyrylcholinesterase (BChE) are considered to be primary regulators of the ACh levels in the brain. Evidence shows that AChE activity decreases in AD, while activity of BChE does not change or even elevate in advanced AD, which suggests a key involvement of BChE in ACh hydrolysis during AD symptoms. Therefore, inhibiting the activity of BChE may be an effective way to control AD associated disorders. In this regard, a series of quinoxaline derivatives 1-17 was synthesized and biologically evaluated against cholinesterases (AChE and BChE) and as well as against achymotrypsin and urease. The compounds 1-17 were found to be selective inhibitors for BChE, as no activity was found against other enzymes. Among the series, compounds 6 (IC50 = 7.7 ± 1.0μM) and 7 (IC50 = 9.7 ± 0.9 μM) were found to be the most active inhibitors against BChE. Their IC50 values are comparable to the standard, galantamine (IC50 = 6.6 ± 0.38 μM). Their considerable BChE inhibitory activity makes them selective candidates for the development of BChE inhibitors. Structure-activity relationship (SAR) of this new class of selective BChE inhibitors has been discussed.

One-pot synthesis of 2-substituted quinoxalines using K10-montmorillonite as heterogeneous catalyst

An efficient one-pot synthesis of 2-substituted quinoxalines from 1,2-diamines and phenacyl bromides is developed using K10-montmorillonite (K10 clay) as a catalyst at 50 C in acetonitrile medium. This method offers an easy route for the synthesis of subs

ANTIMICROBIAL AGENTS

The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

Antibacterial activity of quinoxalines, quinazolines, and 1,5-naphthyridines

Several phenyl substituted naphthalenes and isoquinolines have been identified as antibacterial agents that inhibit FtsZ-Zing formation. In the present study we evaluated the antibacterial of several phenyl substituted quinoxalines, quinazolines and 1,5-naphthyridines against methicillin-sensitive and methicillin-resistant Staphylococcus aureus and vancomycin-sensitive and vancomycin-resistant Enterococcus faecalis. Some of the more active compounds against S. aureus were evaluated for their effect on FtsZ protein polymerization. Further studies were also performed to assess their relative bactericidal and bacteriostatic activities. The notable differences observed between nonquaternized and quaternized quinoxaline derivatives suggest that differing mechanisms of action are associated with their antibacterial properties.