期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 14, 期 12, 页码 3198-3201出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ob00332j
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资金
- Engineering and Physical Sciences Research Council [EP/E000754/1] Funding Source: researchfish
- EPSRC [EP/E000754/1] Funding Source: UKRI
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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