5632-13-3

Usage

Uses

Used in Pharmaceutical Industry:
4-Aminomethylquinoline hydrochloride is used as a key intermediate in the synthesis of 2,4-Diaminoquinazolines and their analogs for the development of treatments for mycobacterial infections. These quinoline-based compounds have shown potential in targeting and inhibiting the growth of mycobacteria, which are responsible for diseases such as tuberculosis.

InChI:InChI=1/C10H10N2.ClH/c11-7-8-5-6-12-10-4-2-1-3-9(8)10;/h1-6H,7,11H2;1H

Upstream product

• 2973-27-5 quinoline-4-carbonitrile 
• 7647-01-0 hydrogenchloride 
• 64-19-7 acetic acid 
• 4363-93-3 quinoline-4-carboxaldehyde 
• 39977-74-7 4-quinolinecarboxaldehyde oxime 
• 126921-64-0 (E)-quinoline-4-carbaldehyde Oxime 
• 1001242-54-1 2-(quinolin-4-ylmethyl)-1H-isoindole-1,3(2H)-dione 
• 3964-04-3 4-bromoquinoline 

Downstream Products

• 858277-78-8 N-acetyl-sulfanilic acid-([4]quinolylmethyl-amide) 
• 76518-57-5 isoquinolin-5-ylmethanol 
• 1173997-56-2 C₁₇H₁₅N₃S 
• 1416568-10-9 4-(3-chloro-2-cyanophenoxy)-N-(4-quinolinylmethyl)benzenesulfonamide 
• 1416568-13-2 4-(phenylmethyl)-N-(4-quinolinylmethyl)benzenesulfonamide 
• 1416568-23-4 4-(2-chloro-4-cyanophenoxy)-N-(quinolinylmethyl)-benzenesulfonamide 
• 1416568-24-5 methyl 2-[4-[[(4-quinolinylmethyl)amino]sulfonyl]phenoxy]-benzoate 
• 1202040-46-7 5-(2,4-bis(trifluoromethyl)phenyl)-1,1-dioxo-2-quinolin-4-ylmethyl-1,2-dihydro-1-benzo[d]isothiazol-3-one 
• 1202040-47-8 5-(2,4-difluorophenyl)-1,1-dioxo-2-quinolin-4-ylmethyl-1,2-dihydro-1-benzo[d]isothiazol-3-one 

Relevant academic research and scientific papers

A quinoline alkaloid rich Quisqualis indica floral extract enhances the bioactivity

A volatile alkaloid quinoline-4-carbonitrile (QCN) was isolated from the floral extract of Quisqualis indica. Major compounds were trans-linalool oxide (1.0, 4.5%), methyl benzoate (1.0, 4.0%), 2,2,6-trimethyl-6-vinyl-tetrahydropyran-3-one (7.4, 17.8%), 2,2,6-trimethyl-6-vinyl-tetrahydropyran-3-ol (1.0, 1.2%), (E,E)-α-farnesene (29.1, 16.1%), QCN (5.7, 1.3%) in live and picked flowers, respectively. Flower compositions were altered due to change in enzymatic reaction at the time of picking. Some rearrangements of oxygenated terpenoids occurred in the process of hydrodistillation to obtain essential oil. Chemical synthesis of QCN and its selectively reduced products derived from QCN were prepared through green reaction process. The catalytic modification of QCN has produced quinoline-4-methylamine; the later compound has shown enhanced bio-activities. QCN and floral extract (absolute) have shown potential anti-inflammatory and antioxidant activities. Besides, floral absolute has shown significant anti-inflammatory and antioxidant activities due to improved QCN (19.7%) content to synergize amongst terpenoids and benzenoids as compared to the essential oil with 1.1% of QCN.

Discovery and optimization of 1-(4-chloro-3-(trifluoromethyl)-phenyl)-3-(2-(amino)pyridin-3-yl)ureas as novel kdr kinase inhibitors

Kinase insert Domain-containing Receptor (KDR) is one of the currently validated targets for anticancer drug discovery and development. Herein, a series of o-amino-arylurea derivatives have been synthesized and evaluated for their kinase inhibitory activity. The optimization on the basis of biological screening and molecular modeling resulted in obvious increase in KDR kinase inhibitory activity compared with the hit compound. Eventually, we identified a potent inhibitor 5a of 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-((quinolin-4-ylmethyl) amino)pyridin-3-yl)urea scaffold against KDR (IC50 = 0.0689 μM), which can serve as good starting point for further KDR inhibitor optimization and development.

Discovery and Optimization of 1-(4-chloro-3-(trifluoromethyl)-phenyl)-3-(2-(amino)pyridin-3-yl)ureas as Novel KDR Kinase Inhibitors

Kinase insert Domain-containing Receptor (KDR) is one of the currently validated targets for anticancer drug discovery and development. Herein, a series of o-amino-arylurea derivatives have been synthesized and evaluated for their kinase inhibitory activity. The optimization on the basis of biological screening and molecular modeling resulted in obvious increase in KDR kinase inhibitory activity compared with the hit compound. Eventually, we identified a potent inhibitor 5a of 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-((quinolin-4-ylmethyl) amino)pyridin-3-yl)urea scaffold against KDR (IC50 = 0.0689 μM), which can serve as good starting point for further KDR inhibitor optimization and development.

SULFONAMIDE ANTHELMINTICS

Disclosed is a method for treating an animal for infection by helmintha which comprises administering to the animal a parasiticidally effective anount of a compound of Formula (1), or a pharmaceutically or veterinarily acceptable salt or a composition com

N- (4 -QUINOLINYLMETHYL) SULFONAMIDE DERIVATIVES AND THEIR USE AS ANTHELMINTICS

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein (1), Q, A, R1, R2, R3 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for treating helminth infections comprising administration to an animal a parasiticidally effective amount of a compound or a composition of the invention.

HETEROCYCLIC COMPOUNDS FOR TREATING HELMINTH INFECTIONS

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein L is (CR13aR13b)t,, CR14=CR14, C≡C, CR15aR15bX, XCR15aR15b, CO, O, S(O)p, NR

PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS

Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.

SUBSTITUTED N-BICYCLICALKYL BICYCLIC CARBOXYAMIDE COMPOUNDS

This invention provides a compound of the formula (I): And their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition compri

Potent inhibitors of tRNA-guanine transglycosylase, an enzyme linked to the pathogenicity of the Shigella bacterium: Charge-assisted hydrogen bonding

Improving inhibition: tRNA-Guanine transglycosylase (TGT) is a newly recognized target to reduce the pathogenicity of disease-causing Shigella bacteria. A potent family of inhibitors of this enzyme has been developed by structure-based design. Crystallographic data and pKa, analysis suggest that the aminoimidazole moiety of the central lin-benzoguanine scaffold is protonated and stabilization of the complexes results from charge-assisted hydrogen bonding. (Figure Presented).