Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase

A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH 2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds 22c, 27b, and 28b inhibited p38α MAP kinase with IC...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.4006-4010
Hauptverfasser: Kim, Dae-Kee, Lim, Jin-Hwi, Lee, Jung A., Dewang, Purushottam M.
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH 2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds 22c, 27b, and 28b inhibited p38α MAP kinase with IC 50 values 27.6, 28, and 31 nM, respectively.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.06.007