465530-68-1Relevant articles and documents
Syntheses, Cholinesterases Inhibition, and Molecular Docking Studies of Pyrido[2,3-b]pyrazine Derivatives
Hameed, Abdul,Zehra, Syeda T.,Shah, Syed J. A.,Khan, Khalid M.,Alharthy, Rima D.,Furtmann, Norbert,Bajorath, Jürgen,Tahir, Muhammad N.,Iqbal, Jamshed
, p. 1115 - 1120 (2015/10/28)
Cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), have a role in cholinergic deficit which evidently leads to Alzheimer's disease (AD). Inhibition of cholinesterases with small molecules is an attractive strategy in AD therapy. This study demonstrates synthesis of pyrido[2,3-b]pyrazines (6a-6q) series, their inhibitory activities against both cholinesterases, AChE and BChE, and molecular docking studies. The bioactivities data of pyrido[2,3-b]pyrazines showed 3-(3′-nitrophenyl)pyrido[2,3-b]pyrazine 6n a potent dual inhibitor among the series against both AChE and BChE with IC50 values of 0.466 ± 0.121 and 1.89 ± 0.05 μm, respectively. The analogues 3-(3′-methylphenyl)pyrido[2,3-b]pyrazine 6c and 3-(3′-fluorophenyl)pyrido[2,3-b]pyrazine 6f were found to be selective inhibition for BChE with IC50 values of 0.583 ± 0.052 μm and AChE with IC50 value of 0.899 ± 0.10 μm, respectively. Molecular docking studies of the active compounds suggested the putative binding modes with cholinesterases. The potent compounds among the series could potentially serves as good leads for the development of new cholinesterase inhibitors. A series of pyrido[2,3-b]pyrazine (6a-6q) derivatives has been synthesized and evaluated for inhibitory activities against cholinesterases; acetylcholinesterase, and butyrylcholinesterase. Molecular docking of active compounds was also performed to suggest the putative binding modes with cholinesterases.
Green oxidations: Titanium dioxide induced tandem oxidation coupling reactions
Jeena, Vineet,Robinson, Ross S.
supporting information; experimental part, (2010/04/22)
The application of titanium dioxide as an oxidant in tandem oxidation type processes is described. Under microwave irradiation, quinoxalines have been synthesized in good yields from the corresponding α-hydroxyketones.
Direct and catalytic synthesis of quinoxaline derivatives from epoxides and ene-1,2-diamines
Antoniotti, Sylvain,Du?ach, Elisabet
, p. 3971 - 3973 (2007/10/03)
We describe here a new synthesis of quinoxaline derivatives by a Bi-catalyzed oxidative coupling of epoxides and ene-1,2-diamines.
