Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin

Here, we describe the development of a series of highly selective PAR4 antagonists with nanomolar potency and selectivity versus PAR1, derived from the indole-based 3. Of these, 9j (PAR4 IC(50) = 445 nM, PAR1 response IC(50) > 30 µM) and 10h (PAR4 IC(50) = 179 nM, PAR1 response IC(50) > 30 µM)...

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Vydáno v:J Med Chem
Hlavní autoři: Temple, Kayla J., Duvernay, Matthew T., Young, Summer E., Wen, Wandong, Wu, Wenjun, Maeng, Jae G., Blobaum, Anna L., Stauffer, Shaun R., Hamm, Heidi E., Lindsley, Craig W.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2016
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5775816/
https://ncbi.nlm.nih.gov/pubmed/27482618
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00928
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