53868-02-3

Basic information

• Product Name: 8-AMinoquinolin-2(1H)-one
• Synonyms: 8-AMinoquinolin-2(1H)-one
• CAS NO: 53868-02-3
• Molecular Formula: C9H8N2O
• Molecular Weight: 160.17262
• Mol File: 53868-02-3.mol
• Article Data: 8

Chemical Properties

• Boiling Point: 417.5±45.0 °C(Predicted)
• Appearance: /
• Density: 1.287±0.06 g/cm3(Predicted)
• PKA: 11.35±0.70(Predicted)
• CAS DataBase Reference: 8-AMinoquinolin-2(1H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 8-AMinoquinolin-2(1H)-one(53868-02-3)
• EPA Substance Registry System: 8-AMinoquinolin-2(1H)-one(53868-02-3)

Safety Data

• Hazardous Substances Data: 53868-02-3(Hazardous Substances Data)

Usage

General Description

8-Aminoquinolin-2(1H)-one, also known as 8-AQ, is a chemical compound with the molecular formula C9H8N2O. It is an organic compound with a quinoline backbone and an amino group at the 8th position. 8-AQ has been studied for its potential pharmaceutical applications, particularly in the field of antimalarial drugs. It has shown promise as a potential anti-malarial agent due to its ability to inhibit the growth of the malaria parasite. Additionally, 8-AQ has also been studied for its potential use in other therapeutic applications, such as in the treatment of neurodegenerative diseases. Overall, 8-Aminoquinolin-2(1H)-one is a compound of interest in the field of medicinal chemistry and drug development.

Upstream product

• 81840-11-1 8-acetylamino-2(1H)-quinolinone 
• 34801-09-7 N-(2-aminophenyl)acetamide 
• 81840-10-0 2-acetylamino-β-ethoxyacryloanilide 
• 7461-12-3 8-Nitroquinolin-2(1H)-one 
• 612-62-4 2-Chloroquinoline 
• 4225-86-9 2-chloro-8-nitroquinoline 

Downstream Products

• 266336-56-5 2-Cyano-4H-imidazo[4,5,1-ij]quinoline-4-one 

Relevant articles and documents

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.

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.