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Issue 12, 2016
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Synthesis of novel and potent vorapaxar analogues

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Abstract

Vorapaxar is a first-in-class PAR-1 antagonistic drug based on the ent-himbacine scaffold. Detailed in this article are enantioselective and racemic routes to various novel vorapaxar analogues. Biological testing revealed these compounds to have moderate to excellent potencies against PAR-1 with the most potent analogue demonstrating an IC50 of 27 nM.

Graphical abstract: Synthesis of novel and potent vorapaxar analogues

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Publication details

The article was received on 11 Dec 2015, accepted on 19 Feb 2016 and first published on 24 Feb 2016


Article type: Paper
DOI: 10.1039/C5OB02541A
Citation: Org. Biomol. Chem., 2016,14, 3264-3274
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    Synthesis of novel and potent vorapaxar analogues

    E. Knight, E. Robinson, N. Smoktunowicz, R. C. Chambers, A. E. Aliev, G. G. Inglis, V. Chudasama and S. Caddick, Org. Biomol. Chem., 2016, 14, 3264
    DOI: 10.1039/C5OB02541A

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