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Himbacine-Derived Thrombin Receptor Antagonists: C(7)-Aminomethyl and C(9a)-Hydroxy Analogues of Vorapaxar
[Image: see text] We have synthesized several C(7)-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a from this series showed excellent PAR-1 activity (K(i) = 5 nM)...
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| Main Authors: | , , , , , , , , |
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| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
American Chemical
Society
2013
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| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4027727/ https://ncbi.nlm.nih.gov/pubmed/24900795 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400452v |
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