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Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors |
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| Authors: | 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 |
| Affiliation: | Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA. ybekkali@rdg.boehringer-ingelheim.com |
| Abstract: | 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 alpha-carbon of the P1 residue. |
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