| 摘要 |
Imidazolone derivatives (I), useful as medicament, are new. Imidazolone derivatives of formula (I), useful as medicament, are new. R 1H, 1-5C alkyl (optionally substituted), aryl or 5 or 6 heterocyclic group (where the aryl and heterocyclic groups comprise optionally one or more substituents occupying any positions); Ar 1aryl group (comprising optionally one or more substituents and two adjacent substituents forming 5 or 6 membered ring (optionally substituted)) or aromatic heterocycle with optionally one or more substituents and/or condensed with 5 or 6 membered aromatic cycle or heteroatoms of N, S or O; R : R 2-S-, R 3-HN-, R 4COHN or Ar 2; R 2linear, branched or cyclic 1-5C alkyl, vinyl or 1-5C vinyl-alkyl, nitrile or 1-5C nitrile-alkyl, aryl or benzyl (all optionally substituted, on one or more carbon atoms, by one or more groups occupying any positions and two adjacent substituents forming 5 or 6-membered ring (optionally substituted)); R 3R 2or H; R 43-5C alkyl; and Ar 2optionally substituted aryl or two adjacent substituents forming 5 or 6-membered ring (optionally substituted). [Image] ACTIVITY : Neuroprotective; Nootropic; Cerebroprotective. MECHANISM OF ACTION : Dual-specificity tyrosine-phosphorylation regulated kinase (DYRK) 1A inhibitor. The ability of (I) to inhibit dual-specificity tyrosine-phosphorylation regulated kinase was tested. The result showed that (I) exhibited an IC 50value of less than 5 ~mM, preferably less than 1 ~mM. |
