Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K

A E Fenwick; B Garnier; A D Gribble; R J Ife; A D Rawlings; J Witherington

doi:10.1016/s0960-894x(00)00626-0

Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K

Bioorg Med Chem Lett. 2001 Jan 22;11(2):195-8. doi: 10.1016/s0960-894x(00)00626-0.

Authors

A E Fenwick¹, B Garnier, A D Gribble, R J Ife, A D Rawlings, J Witherington

Affiliation

¹ Department of Medicinal Chemistry, Smith Kline Beecham Pharmaceuticals, Essex, UK.

PMID: 11206457
DOI: 10.1016/s0960-894x(00)00626-0

Abstract

Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38).

MeSH terms

Binding Sites
Cathepsin K
Cathepsins / antagonists & inhibitors*
Combinatorial Chemistry Techniques
Cysteine Proteinase Inhibitors / chemical synthesis*
Cysteine Proteinase Inhibitors / pharmacology
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Furans / chemistry
Heterocyclic Compounds / chemical synthesis
Heterocyclic Compounds / pharmacology
Humans
Ketones / chemical synthesis
Ketones / pharmacology*
Structure-Activity Relationship
Substrate Specificity

Substances

Cysteine Proteinase Inhibitors
Enzyme Inhibitors
Furans
Heterocyclic Compounds
Ketones
tetrahydrofuran
Cathepsins
CTSK protein, human
Cathepsin K