Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K

A E Fenwick; A D Gribble; R J Ife; N Stevens; J Witherington

doi:10.1016/s0960-894x(00)00627-2

Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K

Bioorg Med Chem Lett. 2001 Jan 22;11(2):199-202. doi: 10.1016/s0960-894x(00)00627-2.

Authors

A E Fenwick¹, A D Gribble, R J Ife, N Stevens, J Witherington

Affiliation

¹ Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.

PMID: 11206458
DOI: 10.1016/s0960-894x(00)00627-2

Abstract

The diastereoselective synthesis of a novel class of cathepsin K inhibitors together with their cathepsin K affinity and stability towards aqueous buffer is reported.

MeSH terms

Buffers
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*
Kinetics
Structure-Activity Relationship

Substances

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