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Himbacine-Derived Thrombin Receptor Antagonists: C(7)-Spirocyclic Analogues of Vorapaxar

[Image: see text] We have synthesized several C(7)-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar. Compound 5c from this series showed excellent PAR-1 activity...

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Detalhes bibliográficos
Main Authors: Chelliah, Mariappan V., Eagen, Keith, Guo, Zhuyan, Chackalamannil, Samuel, Xia, Yan, Tsai, Hsingan, Greenlee, William J., Ahn, Ho-Sam, Kurowski, Stan, Boykow, George, Hsieh, Yunsheng, Chintala, Madhu
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2014
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027741/
https://ncbi.nlm.nih.gov/pubmed/24900880
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500008w
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