Jump to main content
Jump to site search

Issue 12, 2016
Previous Article Next Article

Synthesis of novel and potent vorapaxar analogues

Author affiliations


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

Back to tab navigation

Supplementary files

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
Author version
Download author version (PDF)
Citation: Org. Biomol. Chem., 2016,14, 3264-3274

  •   Request permissions

    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

Search articles by author