Ontology highlight
ABSTRACT:
SUBMITTER: Lee S
PROVIDER: S-EPMC4027540 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Lee Sunkyung S Song Jong-Hwan JH Park Chul Min CM Kim Jin-Seok JS Jeong Ji-Hye JH Cho Woo-Young WY Lim Dong-Chul DC
ACS medicinal chemistry letters 20130910 11
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 pot ...[more]