1207531-98-3Relevant articles and documents
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38α mitogen-activated protein kinase inhibitors
Koch, Pierre,Jahns, Hartmut,Schattel, Verena,Goettert, Marcia,Laufer, Stefan
, p. 1128 - 1137 (2010)
Various substituted 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4-yl)quinoxalines and 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4-yl)pyridopyrazines were synthesized as novel p38α MAP kinase inhibitors via different short synthetic strategies with high variation possibilities. The formation of the quinoxaline/ pyridopyrazine core was achieved from α-diketones and o-phenylenediamines/ α-diaminopyridines under microwave irradiation. Introduction of an amino moiety at the pyridine C2 position of the 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4- yl)quinoxalines led to compounds showing potent enzyme inhibition down to the double-digit nanomolar range (6f; IC50 = 81 nM). Replacement of the quinoxaline core with pyrido[2,3-b]pyrazine gave compound 9e with superior p38α MAP kinase inhibition (IC50= 38 nM).
