28419-74-1

Usage

Uses

Used in Pharmaceutical Research:
2-(1H-PYRROLO[3,2-B]PYRIDIN-3-YL)ETHANAMINE is used as a research chemical for exploring its potential interactions with neurotransmitter receptors in the brain. Its unique structure may offer insights into the development of new therapeutic agents for neurological disorders.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 2-(1H-PYRROLO[3,2-B]PYRIDIN-3-YL)ETHANAMINE is used as a lead compound for the design and synthesis of new drugs targeting specific receptors or pathways in the nervous system. Its structural features can be modified to optimize pharmacological activity and selectivity.
Used in Neurotransmitter Receptor Studies:
2-(1H-PYRROLO[3,2-B]PYRIDIN-3-YL)ETHANAMINE is used as a tool compound in studies aimed at understanding the mechanisms of neurotransmitter receptor interactions. Its ability to bind to these receptors can provide valuable information on receptor function and the development of drugs targeting these receptors.
Used in Drug Discovery:
In the drug discovery process, 2-(1H-PYRROLO[3,2-B]PYRIDIN-3-YL)ETHANAMINE is used as a starting point for the identification of novel therapeutic agents with potential applications in various diseases and conditions. Its unique chemical structure can be a basis for the development of new drugs with improved efficacy and safety profiles.

Upstream product

• 23612-34-2 N,N-dimethyl-1-(1H-pyrrolo[3,2-b]pyridin-3-yl)methanamine 
• 554453-19-9 2-(1H-pyrrolo[3,2-b]pyridin-3-yl)acetonitrile 
• 272-49-1 1H-pyrrolo[3,2-b]pyridine 
• 24509-72-6 2-(1H-pyrrolo[3,2-b]pyridin-3-yl)-acetamide 
• 1378810-11-7 2-oxo-2-(1H-pyrrolo[3,2-b]pyridin-3-yl)acetamide 

Downstream Products

• 1312891-85-2 (E)-3-(4-{[2-(1H-pyrrolo[3,2-b]pyridin-3-yl)ethylamino]methyl}phenyl)acrylic acid methyl ester 
• 1312891-47-6 (E)-N-hydroxy-3-(4-{[2-(1H-pyrrolo[3,2-b]pyridin-3-yl)ethylamino]methyl}phenyl)acrylamide 

Relevant academic research and scientific papers

Synthesis and SAR of the antistaphylococcal natural product nematophin from Xenorhabdus nematophila

The repeated and improper use of antibiotics had led to an increased number of multiresistant bacteria. Therefore, new lead structures are needed. Here, the synthesis and an expanded structure–activity relationship of the simple and antistaphylococcal amide nematophin from Xenorhabdus nematophila and synthetic derivatives are described. Moreover, the synthesis of intrinsic fluorescent derivatives, incorporating azaindole moieties was achieved for the first time.

INDOLE AHR INHIBITORS AND USES THEREOF

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors

Histone deacetylase (HDAC) inhibitors have shown promise in treating various forms of cancer. However, many HDAC inhibitors from diverse structural classes have been associated with QT prolongation in humans. Inhibition of the human ether a-go-go related gene (hERG) channel has been associated with QT prolongation and fatal arrhythmias. To determine if the observed cardiac effects of HDAC inhibitors in humans is due to hERG blockade, a highly potent HDAC inhibitor devoid of hERG activity was required. Starting with dacinostat (LAQ824), a highly potent HDAC inhibitor, we explored the SAR to determine the pharmacophores required for HDAC and hERG inhibition. We disclose here the results of these efforts where a high degree of pharmacophore homology between these two targets was discovered. This similarity prevented traditional strategies for mitigating hERG binding/modulation from being successful and novel approaches for reducing hERG inhibition were required. Using a hERG homology model, two compounds, 11r and 25i, were discovered to be highly efficacious with weak affinity for the hERG and other ion channels.

ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, Q, G, Ar, m, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Azaindolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands

The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.