55931-63-0

Upstream product

• 91494-87-0 [4-(2-chloro-phenyl)-piperazin-1-yl]-acetonitrile 
• 39512-50-0 N-(o-Chlorophenyl)piperazine 
• 75000-28-1 2-(2-(4-(2-chlorophenyl)-piperazin-1-yl)-ethyl)-isoindoline-1,3-dione 

Downstream Products

• 112822-49-8 4-(3-{2-[4-(2-Chloro-phenyl)-piperazin-1-yl]-ethyl}-ureido)-furan-3-carboxylic acid 
• 1221290-77-2 N-{2-[4-(2-chlorophenyl)piperazin-1-yl]ethyl}-2-quinoline carboxamide 
• 1221290-89-6 N-{2-[4-(2-chlorophenyl)piperazin-1-yl]ethyl}-3-quinoline carboxamide 
• 1221290-67-0 N-{2-[4-(2-chlorophenyl)piperazin-1-yl]ethyl}-2-quinoxaline carboxamide 
• 1240266-50-5 C₂₅H₃₁ClN₄O*ClH 
• 1608157-09-0 N⁵-(2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl)-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine 
• 112822-33-0 3-[2-[4-(2-chlorophenyl)piperazin-1-yl]ethyl]furo[3,4-d]pyrimidine-2,4-dione 

Relevant academic research and scientific papers

Small-Molecule Inhibition of the UNC119–Cargo Interaction

N-Terminal myristoylation facilitates membrane binding and activity of proteins, in particular of Src family kinases, but the underlying mechanisms are only beginning to be understood. The chaperones UNC119A/B regulate the cellular distribution and signal

Binding kinetics of ZM241385 derivatives at the human adenosine A 2A receptor

Classical drug design and development rely mostly on affinity- or potency-driven structure-activity relationships (SAR). Thus far, a given compound's binding kinetics have been largely ignored, the importance of which is now being increasingly recognized. In the present study, we performed an extensive structure-kinetics relationship (SKR) study in addition to a traditional SAR analysis at the adenosine A2A receptor (A 2AR). The ensemble of 24 A2AR compounds, all triazolotriazine derivatives resembling the prototypic antagonist ZM241385 (4-(2-((7-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino) ethyl)phenol), displayed only minor differences in affinity, although they varied substantially in their dissociation rates from the receptor. We believe that such a combination of SKR and SAR analyses, as we have done with the A 2AR, will have general importance for the superfamily of G protein-coupled receptors, as it can serve as a new strategy to tailor the interaction between ligand and receptor. Above and beyond: Insight into the binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor has provided additional information beyond a traditional structure-activity relationship (SAR) analysis. The strategy, combining a structure-kinetics relationship investigation and SAR, can serve as an important tool for more directed medicinal chemistry efforts in the future.

Chemical modifications on 4-arylpiperazine-ethyl carboxamide derivatives differentially modulate affinity for 5-HT1A, D4.2, and α2A receptors: Synthesis and in vitro radioligand binding studies

A series of substituted 4-aryl-piperazine-ethyl heteroarylcarboxamides were prepared and tested in in vitro radioligand binding studies. The presence of a quinoxaline has a favourable impact in terms of serotonin 5-HT1A versus dopamine D4.2 receptor selectivity. Compounds with a 3-CF3 group at the distal phenyl ring are the most effective in terms of affinity and selectivity for 5-HT1A versus D4.2 receptors. A 4-phenyl-1,2,3,6- tetrahydropyridine in place of the corresponding 4-phenyl-piperazine side chain is also favourable not only for the affinity for 5-HT1A and D4.2 receptors but also in some cases for α2A-adrenoceptors.

Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers

T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs

Phenylpiperazinylalkylamino substituted pyridazinones as potent α1 adrenoceptor antagonists

QSAR models have been used for designing a series of compounds characterized by a N-phenylpiperazinylalkylamino moiety linked to substituted pyridazinones, which have been synthesized. Measurements of the binding affinities of the new compounds toward the