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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Главные авторы: Chelliah, Mariappan V., Chackalamannil, Samuel, Xia, Yan, Greenlee, William J., Ahn, Ho-Sam, Kurowski, Stan, Boykow, George, Hsieh, Yunsheng, Chintala, Madhu
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2013
Online-ссылка: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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