83027-13-8

Usage

Uses

AMN082 dihydrochloride is a selective agonist at mGluR-7.

Biological Activity

The first selective mGlu 7 agonist. Potently inhibits cAMP accumulation and stimulates GTP γ S binding in recombinant cells and on membranes expressing mGlu 7 (EC 50 = 64-290 nM). Selective over other mGluR subtypes and selected ionotropic glutamate receptors up to 10 μ M. Acts via a novel allosteric site and is orally active and brain penetrant. Reduces haloperidol-induced catalepsy in rats.

Upstream product

• 104-71-2 N,N'-bis(benzyliden)ethylendiamine 
• 64042-50-8 N,N'-bis(α-phenylbenzylidene)ethylenediamine 
• 119-61-9 benzophenone 
• 107-15-3 ethylenediamine 
• 141734-22-7 N¹,N²-dibenzhydrylethane-1,2-diimine 

Downstream Products

• 1370700-79-0 1,3-dibenzhydrylimidazolinium chloride 

Relevant academic research and scientific papers

Copper-Catalyzed Propargylation of Nitroalkanes

Using a commercially available, inexpensive, and abundant copper catalyst system, an efficient α-functionalization of nitroalkanes with propargyl bromides is now established. This mild and robust method is highly functional group tolerant and provides straightforward access to complex secondary and tertiary homopropargylic nitroalkanes. Moreover, the utility of these α-propargylated nitroalkanes is demonstrated through downstream functionalization to biologically relevant, five-membered N-heterocycles such as pyrroles and 2-pyrrolines.

Design of bis-NHC Ru-complexes featuring diarylmethylene N-substituents for olefin metathesis

New ruthenium indenylidene complexes containing N-heterocyclic carbene (NHC) ligands were synthesized and evaluated in olefin metathesis. The presence of two symmetrical saturated NHCs featuring N-diarylmethylene fragments (R= H, OMe or F) led to robust ruthenium precatalysts with a good latency. A kinetic study was investigated showing that a thermal stimulus (>60 °C) is required to reach an efficient catalytic initiation. Interestingly, a slight electronic effect was observed depending on the presence of an electron-donating or –withdrawing group within the diarylmethylene moiety. These complexes showed good activity at 1 mol% of catalyst loading in selected ring-closing metathesis (RCM) and cross-metathesis (CM) transformations.

Imidazolinium chloride salts bearing wingtip groups: Synthesis, molecular docking and metabolic enzymes inhibition

A series of symmetrical imidazolinium chloride salts bearing secondary N-alkyl substituents were synthesized in good yield by the reaction of N,N′-dialkylethane-1,2-diamines and HC(OEt)3 in the presence of NH4Cl. These salts were characterized by spectroscopic methods. All compounds were tested as enzyme inhibitory agents. These novel symmetrical imidazolinium chloride salts derivatives (3a-h) effectively inhibited the cytosolic hCA I and hCA II, BChE, α-glycosidase and AChE with Ki values in the range of 18.41–121.73 nM for hCA I, 12.50–63.12 nM for hCA II, 3.72–34.58 nM for AChE, 5.50–32.36 nM for BChE, and 94.72–364.51 nM for α-glycosidase, respectively. CA isoenzymes play a crucial roles including acid-base balance homeostasis by excreting and secreting protons (H+) due to the CO2 hydration, HCO3 ? reabsorption mechanisms, and renal NH4 + output. Also, the molecular modeling is an implementation for estimation of the binding proximity of symmetrical imidazolinium chloride salts bearing secondary wingtip groups and their inhibition mechanisms and kinetics in atomic levels at the catalytic domains.

Electrochemical Reduction of Di-Schiff Bases. Synthesis of Piperazines, Indoloindoles, Diazepines, and Diazocines

The electrochemical reduction of a series of di-Schiff bases had led to examples where products representing reduction, cyclization, and transannular cyclization are found.Useful synthetic pathways for piperazines, indoloindoles, diazepines, and diazocines are described.