Bioorganic and Medicinal Chemistry Letters p. 2465 - 2469 (2007)
Update date:2022-08-03
Topics:
Bekkali, Younes
Thomson, David S.
Betageri, Raj
Emmanuel, Michel J.
Hao, Ming-Hong
Hickey, Eugene
Liu, Weimin
Patel, Usha
Ward, Yancey D.
Young, Erick R.R.
Nelson, Richard
Kukulka, Alison
Brown, Maryanne L.
Crane, Kathy
White, Della
Freeman, Dorothy M.
Labadia, Mark E.
Wildeson, Jessi
Spero, Denice M.
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.
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Doi:10.1246/cl.2007.528
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