Robinson, E;
Knight, E;
Smoktunowicz, N;
Chambers, RC;
Inglis, GG;
Chudasama, V;
Caddick, S;
(2016)
Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability.
Organic & Biomolecular Chemistry
(14)
pp. 3198-3201.
10.1039/c6ob00332j.
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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.
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