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Bioorg Med Chem Lett. 2010 Apr 1;20(7):2375-8. doi: 10.1016/j.bmcl.2010.01.104. Epub 2010 Feb 1.

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions.

Author information

1
Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. Jwiener1@its.jnj.com

Abstract

A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR investigations of the P3, P4, and P5 regions are described. In particular, 4-fluoropiperidine is identified as a competent P3 binding element when utilized in conjunction with a (S)-2-hydroxypropyl linker-containing P5 moiety and oxamide or sulfonamide P4 substitution.

PMID:
20171097
DOI:
10.1016/j.bmcl.2010.01.104
[Indexed for MEDLINE]

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