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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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| Publicado no: | J Med Chem |
|---|---|
| Main Authors: | , , , , , , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2016
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| Assuntos: | |
| Acesso em linha: | 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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