1579953-07-3

Upstream product

• 1579953-02-8 C₂₁H₂₆BrNO₃ 
• 1579952-97-8 C₃₀H₃₂F₃NO₄ 
• 618386-50-8 C₂₈H₂₈F₃NO₃ 
• 1518836-90-2 C₂₉H₃₀F₃NO₃ 
• 1579953-05-1 (1R,3aR,4aR,4'S,8aR,9S,9aS)-9-((E)-2-(5-bromopyridin-2-yl)vinyl)-1-methyloctahydro-1H-spiro[naphtho[2,3-c]furan-6,4'-oxazolidine]-2',3(7H)-dione 
• 214360-47-1 2-(5,5-dimethyl-[1,3,2]dioxaborinan-2-yl)-benzonitrile 
• 1579953-04-0 ((1R,3aR,4aS,6R,8aR,9S,9aS)-9-((E)-2-(5-bromopyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl)methyl carbamate 
• 1579952-99-0 ((1R,3aR,4aS,6R,8aR,9S,9aS)-9-((E)-2-(5-bromopyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl)methyl acetate 
• 1579952-98-9 ((1R,3aR,4aS,6R,8aR,9S,9aS)-9-formyl-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl)methyl acetate 
• 1579952-94-5 (3R,3aS,4S,4aR,7R,8aS,9aR)-7-(hydroxymethyl)-3-methyl-4-((E)-2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)decahydronaphtho[2,3-c]furan-1(3H)-one 

Relevant academic research and scientific papers

Himbacine-derived thrombin receptor antagonists: C7-Spirocyclic analogues of vorapaxar

We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar. Compound 5c from this series showed excellent PAR-1 activity (K i = 5.1 nM). We also present a model of these spirocyclic compounds docked to the PAR-1 receptor based on the X-ray crystal structure of vorapaxar bound to PAR-1 receptor. This model explains some of the structure-activity relationships in this series.