Synthesis of novel and potent vorapaxar analoguesElectronic supplementary information (ESI) available: 1H and 13C NMR spectra of all novel compounds. See DOI: 10.1039/c5ob02541a

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 th...

Full description

Saved in:
Bibliographic Details
Main Authors Knight, Emily, Robinson, Eifion, Smoktunowicz, Natalia, Chambers, Rachel C, Aliev, Abil E, Inglis, Graham G, Chudasama, Vijay, Caddick, Stephen
Format Journal Article
Published 15.03.2016
Online AccessGet full text

Cover

More Information
Summary: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 IC 50 of 27 nM. Unlocking novel and potent vorapaxar analogues by functionalisation of previously unexplored positions on the parent vorapaxar scaffold.
Bibliography:1
13
Electronic supplementary information (ESI) available
H and
C NMR spectra of all novel compounds. See DOI
10.1039/c5ob02541a
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob02541a