111770-91-3Relevant articles and documents
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide
Liu, Jun,Sun, Bin,Zhao, Xiaoyu,Xing, Jie,Gao, Yanhui,Chang, Wenqiang,Ji, Jianbo,Zheng, Hongbo,Cui, Changyi,Ji, Aiguo,Lou, Hongxiang
, p. 7166 - 7185 (2017)
Protease-activated receptor-1 (PAR1), a G-protein-coupled receptor, plays a critical role in thrombin-mediated platelet aggregation. It is regarded as a promising antithrombosis target that is unlikely to result in bleeding. Here, we describe the synthesi
Discovery of octahydroindenes as PAR1 antagonists
Lee, Sunkyung,Song, Jong-Hwan,Park, Chul Min,Kim, Jin-Seok,Jeong, Ji-Hye,Cho, Woo-Young,Lim, Dong-Chul
supporting information, p. 1054 - 1058 (2013/12/04)
Octahydroindene was identified as a novel scaffold for protease activated receptor 1 (PAR1) antagonists. Herein, the 2-position (C2) was explored for structure-activity relationship (SAR) studies. Compounds 14, 19, and 23b showed IC50 values of 1.3, 8.6, and 2.7 nM in a PAR1 radioligand binding assay, respectively, and their inhibitory activities on platelet activation were comparable to that of vorapaxar in a platelet rich plasma (PRP) aggregation assay. This series of compounds showed high potency and no significant cytotoxicity; however, the compounds were metabolically unstable in both human and rat liver microsomes. Current research efforts are focused on optimizing the compounds to improve metabolic stability and physicochemical properties as well as potency.
PROCESS FOR PREPARING 1-(6-METHYLPYRIDIN-3-YL)-2-[4-(METHYLSULFONYL)PHENYL]ETHANONE, AN INTERMEDIATE OF ETORICOXIB
-
Page/Page column 4, (2012/09/22)
A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.