58336-33-7

Usage

Uses

Used in Pharmaceutical Industry:
7-Amino-2(1H)-quinolinone is used as a therapeutic agent for its potential antitumor, anti-inflammatory, antibacterial, and anticancer properties. It is valued for its ability to modulate various biological activities, making it a promising candidate for the development of new drugs and treatments.
Used in Scientific Research:
In the field of scientific research, 7-Amino-2(1H)-quinolinone is used as a compound of interest for studying its chemical properties and potential interactions with biological systems. Researchers explore its applications in understanding disease mechanisms and developing targeted therapies.
Used in Drug Development:
7-Amino-2(1H)-quinolinone is utilized in drug development as a lead compound for the creation of new pharmaceuticals. Its diverse biological activities suggest that it could be a key component in the formulation of medications for a variety of health conditions, particularly those related to cancer and inflammation.

InChI:InChI=1/C9H8N2O/c10-7-3-1-6-2-4-9(12)11-8(6)5-7/h1-5H,10H2,(H,11,12)

Upstream product

• 613-51-4 7-nitroquinoline 
• 102170-39-8 4-amino-2-nitrobenzaldehyde 
• 635-46-1 1,2,3,4-tetrahydroisoquinoline 
• 30450-62-5 7-nitro-1,2,3,4-tetrahydro-quinoline 
• 14753-17-4 7-Nitro-chinolin-1-oxyd 
• 75755-37-2 7-nitroquinoline-2(1H)-one 
• 1116135-32-0 7-amino-3-chloro-3,4-dihydroquinolin-2(1H)-one 
• 119-32-4 4-Methyl-3-nitroanilin 
• 100796-40-5 4-acetylamino-1-diacetoxymethyl-2-nitro-benzene 
• 108-45-2 m-phenylenediamine 
• 502143-68-2 7-amino-2-hydroxy-quinoline-4-carboxylic acid ethyl ester 
• 528-75-6 2,4-dinitrobenzaldehyde 
• 85818-66-2 2,4-dinitro-cinnamic acid 
• 98879-66-4 4-amino-2-nitro-trans-cinnamic acid 

Downstream Products

• 70500-72-0 quinoline-2,7-diol 

Relevant academic research and scientific papers

Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift

Among a series of benzopyridone-based scaffolds investigated as human transient receptor potential vanilloid 1 (TRPV1) ligands, two isomeric benzopyridone scaffolds demonstrated a consistent and distinctive functional profile in which 2-oxo-1,2-dihydroquinolin-5-yl analogues (e.g., 2) displayed high affinity and potent antagonism, whereas 1-oxo-1,2-dihydroisoquinolin-5-yl analogues (e.g., 3) showed full agonism with high potency. Our computational models provide insight into the agonist-antagonist boundary of the analogues suggesting that the Arg557 residue in the S4-S5 linker might be important for sensing the agonist binding and transmitting signals. These results provide structural insights into the TRPV1 and the protein-ligand interactions at a molecular level.

N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties

Urea transporters (UTs) have been identified as new targets for diuretics. Functional deletion of UTs led to urea-selective urinary concentrating defects with relative salt sparing. In our previous study, a UT inhibitor with a diarylamide scaffold, which is denoted as 11a, was demonstrated as the first orally available UT inhibitor. However, the oral bioavailability of 11a was only 4.38%, which obstructed its clinical application. In this work, by replacing the nitro group of 11a with an acetyl group, 25a was obtained. Compared with 11a, 25a showed a 10 times stronger inhibitory effect on UT-B (0.14 μM vs. 1.41 μM in rats, and 0.48 μM vs. 5.82 μM in mice) and a much higher inhibition rate on UT-A1. Moreover, the metabolic stability both in vitro and in vivo and the drug-like properties (permeability and solubility) of 25a were obviously improved compared with those of 11a. Moreover, the bioavailability of 25a was 15.18%, which was 3 times higher than that of 11a, thereby resulting in significant enhancement of the diuretic activities in rats and mice. 25a showed excellent potential for development as a promising clinical diuretic candidate for targeting UTs to treat diseases that require long-term usage of diuretics, such as hyponatremia.

CONDENSED HETEROCYCLIC 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, A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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.

4'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): formula (I) wherein Cy is selected from formula (Il) and wherein R1, R2, R3, Q, G, Ar, m, n and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

3' SUBSTITUTED 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 Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

BENZAMIDE DERIVATIVE OR SALT THEREOF

There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder