Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles

FX Tavares, DN Deaton, AB Miller, LR Miller…

Index: Tavares, Francis X.; Deaton, David N.; Miller, Aaron B.; Miller, Larry R.; Wright, Lois L. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3891 - 3895

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Citation Number: 14

Abstract

Ketoheterocyclic inhibitors of cathepsin K have been disclosed. SAR of potency enhancing P2–P3 groups coupled with ketoheterocyclic warheads to provide cathepsin K inhibitors have been described. In addition, a novel route to access α-ketothiazoles using a key thioamide functionality has been disclosed. The mild method employed allows for the presence of diverse functional groups, such as amide and carbamate functionalities, ...