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Issue 12, 2016
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Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability

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Abstract

The discontinuation of PAR-1 antagonist RWJ-58259 beyond use as a biological probe is most likely due to it's short half-life in vivo. However, retention of significant in vivo activity beyond the point where most of the RWJ-58259 had been consumed implies the generation of an active metabolite. Herein we describe the biological activity of a predicted metabolite of RWJ-58259 and the synthesis of analogues designed to enhance the metabolic stability of RWJ-58259.

Graphical abstract: Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability

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Supplementary files

Article information


Submitted
10 Feb 2016
Accepted
25 Feb 2016
First published
25 Feb 2016

Org. Biomol. Chem., 2016,14, 3198-3201
Article type
Communication
Author version available

Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability

E. Robinson, E. Knight, N. Smoktunowicz, R. C. Chambers, G. G. Inglis, V. Chudasama and S. Caddick, Org. Biomol. Chem., 2016, 14, 3198
DOI: 10.1039/C6OB00332J

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