116632-53-2

Usage

Uses

Used in Pharmaceutical Industry:
7-Bromoquinolin-2-amine is used as a key intermediate in the synthesis of various pharmaceutical drugs for the treatment of different diseases and medical conditions. Its unique chemical structure and properties contribute to the development and production of effective drugs.
Used in Medicinal Chemistry and Drug Discovery Research:
In the field of medicinal chemistry and drug discovery, 7-Bromoquinolin-2-amine serves as an essential component in research and development activities. Its unique properties and chemical structure make it a promising candidate for the creation of innovative drugs and therapeutic agents, enhancing the discovery of novel treatments and improving patient outcomes.

InChI:InChI=1/C9H7BrN2/c10-7-3-1-6-2-4-9(11)12-8(6)5-7/h1-5H,(H2,11,12)

Upstream product

• 99455-15-9 7-bromo-2-chloro-quinoline 
• 99465-10-8 7-bromo-quinolin-2-ol 

Relevant academic research and scientific papers

SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5

The disclosure is directed to methods of treating disease using compounds of Formula (I).

Selective Inhibitors Of Protein Arginine Methyltransferase 5 (PRMT5)

The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors

Neuronal nitric oxide synthase (nNOS) inhibition is a promising strategy to treat neurodegenerative disorders, but the development of nNOS inhibitors is often hindered by poor pharmacokinetics. We previously developed a class of membrane-permeable 2-amino

From fragment screening to in vivo efficacy: Optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (bace1)

Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was identified as an initial hit for BACE1. Further SAR development was supported by X-ray structures of BACE1 cocrystallized with various ligands and molecular modeling studies to expedite the discovery of potent compounds. These strategies enabled us to integrate the C-3 side chain on 2-aminoquinoline 1 extending deep into the P2′ binding pocket of BACE1 and enhancing the ligand's potency. We were able to improve the BACE1 potency to subnanomolar range, over 106-fold more potent than the initial hit (900 μM). Further elaboration of the physical properties of the lead compounds to those more consistent with good blood-brain barrier permeability led to inhibitors with greatly improved cellular activity and permeability. Compound 59 showed an IC50 value of 11 nM on BACE1 and cellular activity of 80 nM. This compound was advanced into rat pharmacokinetic and pharmacodynamic studies and demonstrated significant reduction of Aβ levels in cerebrospinal fluid (CSF).