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Synthesis of novel and potent vorapaxar analogues

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. Green open access

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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.

Type: Article
Title: Synthesis of novel and potent vorapaxar analogues
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1039/c5ob02541a
Publisher version: http://dx.doi.org/10.1039/c5ob02541a
Language: English
Additional information: Copyright © Royal Society of Chemistry 2016
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Respiratory Medicine
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/1476428
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