Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors
John S Debenham1, Thomas H Graham, Andreas Verras
1Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
Bioorganic & Medicinal Chemistry Letters
|October 26, 2013
Abstract:
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagement in mouse plasma 20 h post oral dose.
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