Knight, E;
Robinson, E;
Smoktunowicz, N;
Chambers, RC;
Aliev, AE;
Inglis, GG;
Chudasama, V;
(2016)
Synthesis of novel and potent vorapaxar analogues.
Organic & Biomolecular Chemistry
, 14
(12)
pp. 3264-3274.
10.1039/c5ob02541a.
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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.
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