5632-13-3Relevant articles and documents
A quinoline alkaloid rich Quisqualis indica floral extract enhances the bioactivity
Rout, Prasant Kumar,Kumar, Prashant,Rao, Y. Ramachandra,Kumar, Anant,Bawankule, Dnyaneshwar U.,Singh, Ruchi,Singh, Kijay Bahadur,Chanotiya, Chandan Singh,Naik
, p. 1632 - 1638 (2019/07/12)
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
Jiao, Yu,Huang, Fei,Xu, Pengfei,Zhang, Yanmin,Yang, Shangyan,Zhang, Danfeng,Lu, Tao,Tang, Weifang
, p. 328 - 337 (2016/10/12)
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.
N- (4 -QUINOLINYLMETHYL) SULFONAMIDE DERIVATIVES AND THEIR USE AS ANTHELMINTICS
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Page/Page column 43; 44, (2013/06/27)
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.