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Synthesis of new series of quinoxaline based MAO-inhibitors and docking studies

Serine N. Khattab ; Seham Y. Hassan ; Adnan A. Bekhit ; Abdel Moneim El Massry ; Vratislav Langer (Institutionen för kemi- och bioteknik, Oorganisk miljökemi) ; Adel Amer
European Journal of Medicinal Chemistry (0223-5234). Vol. 45 (2010), 10, p. 4479-4489.
[Artikel, refereegranskad vetenskaplig]

A series of 2-benzyl-3-(2-arylidenehydrazinyl)quinoxalines 3, 4-benzyl-1-aryl-[1,2,4]triazolo[4,3-a]quinoxalines 4 and phenyl(1-aryl-[1,2,4]triazolo[4,3-a]quinoxalin-4-yl)methanones 5 analogues were synthesized and investigated for their monoamine oxidase (MAO) inhibitory property. The inhibition profile was found to be competitive for compounds 3k, 3m, 5f and 5n with MAO-A selectivity. Observation of the docked positions of these compounds revealed interactions with many residues previously reported to have an effect on the inhibition of the enzyme. The structural features of the new compounds have been determined from the microanalytical, IR, 1H, 13C NMR spectral studies and X-ray crystalography.

Nyckelord: Quinoxalines, [1,2,4]Triazolo[4,3-a]quinoxalines, Oxidation, Oxidative cyclization, Monoamine oxidase inhibitors



Denna post skapades 2010-09-07. Senast ändrad 2010-10-14.
CPL Pubid: 125765

 

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Institutioner (Chalmers)

Institutionen för kemi- och bioteknik, Oorganisk miljökemi (2005-2014)

Ämnesområden

Organisk syntes
Bioorganisk kemi
Läkemedelskemi

Chalmers infrastruktur