Discovery and parallel synthesis of a new class of cathepsin K inhibitors

R A Smith; A Bhargava; C Browe; J Chen; J Dumas; H Hatoum-Mokdad; R Romero

doi:10.1016/s0960-894x(01)00600-x

Discovery and parallel synthesis of a new class of cathepsin K inhibitors

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2951-4. doi: 10.1016/s0960-894x(01)00600-x.

Authors

R A Smith¹, A Bhargava, C Browe, J Chen, J Dumas, H Hatoum-Mokdad, R Romero

Affiliation

¹ Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. roger.smith.b@bayer.com

PMID: 11677133
DOI: 10.1016/s0960-894x(01)00600-x

Abstract

Peptidomimetic aminomethyl ketones have been identified as a new class of cathepsin K inhibitors. Traditional and high-speed parallel synthesis techniques were applied to investigate this series. Structure-activity relationships were established, and certain analogues were characterized with IC(50) values in the range 200-500 nM.

MeSH terms

Cathepsin K
Cathepsins / antagonists & inhibitors*
Cysteine Proteinase Inhibitors / chemical synthesis*
Cysteine Proteinase Inhibitors / chemistry
Drug Design
Inhibitory Concentration 50
Ketones / chemistry*
Kinetics
Molecular Mimicry
Structure-Activity Relationship

Substances

Cysteine Proteinase Inhibitors
Ketones
Cathepsins
Cathepsin K