281217-45-6Relevant articles and documents
Synthesis of 3-oxoazacyclohept-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K
Taillier, Catherine,Hameury, Thomas,Bellosta, Veronique,Cossy, Janine
, p. 549 - 554 (2007/10/03)
The ring-closing metathesis allows the formation of 3-oxoazacyclohept-4-enes from but-3-enamine. By using this methodology, the synthesis of an inhibitor of cathepsin K was achieved in 10 steps from but-3-enamine.
Azepanone-based inhibitors of human and rat cathepsin K
Marquis,Ru,LoCastro,Zeng,Yamashita,Oh,Erhard,Davis,Tomaszek,Tew,Salyers,Proksch,Ward,Smith,Levy,Cummings,Curtis Haltiwanger,Trescher,Wang,Hemling,Quinn,Cheng,Lin,Smith,Janson,Zhao,McQueney,D'Alessio,Lee,Marzulli,Dodds,Blake,Hwang,James,Gress,Bradley,Lark,Gowen,Veber
, p. 1380 - 1395 (2007/10/03)
The synthesis, in vitro activities, and pharmacokinetics of a series of azepanone-based inhibitors of the cysteine protease cathepsin K (EC 3.4.22.38) are described. These compounds show improved configurational stability of the C-4 diastereomeric center
