1107621-02-2Relevant articles and documents
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-Ribose) polymerase-1 inhibitors
Zhang, Wen-Ting,Ruan, Jin-Lan,Wu, Peng-Fei,Jiang, Feng-Chao,Zhang, Li-Na,Fang, Wei,Chen, Xiang-Long,Wang, Yue,Cao, Bao-Shuai,Chen, Gang-Ying,Zhu, Yi-Jing,Gu, Jun,Chen, Jian-Guo
, p. 718 - 725 (2009)
A series of novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors were designed within 2-aminothiazole analogues (4-10) based on a constructed three-dimensional pharmacophore model. After synthesis, the inhibitory effect on PARP-1 activity and the cytoprotective action of these compounds were tested and evaluated. Among them, compounds 4-6 and 10 appeared to be potent PARP-1 inhibitors with IC50 values less than 1 μM, which had been perfectly predicted by pharmacophore model. These compounds proved to be highly potent against cell injury induced by H2O2 and oxygen-glucose deprivation (OGD) in PC12 cells. These novel 2-aminothiazole analogues are potentially applicable as neuroprotective agents for the treatment of neurological diseases.