[摘要]：A series of novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors were designed within 2-aminothiazole analogs based on a constructed three-dimensional pharmacophore model. Then, the inhibitory effect on PARP-1 activity and the cytoprotective action of these compds. were tested and evaluated. Among them, four compds. appeared to be potent PARP-1 inhibitors with IC50 values less than 1 mM, which had been perfectly predicted by pharmacophore model. These compds. proved to be highly potent against cell injury induced by H2O2 and oxygen-glucose deprivation (OGD) in PC12 cells. These 2-aminothiazole analogs are potentially applicable as neuroprotective agents for the treatment of neurol. diseases.
