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

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

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

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2951-4.

PubMed ID

11677133 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N2-[(Benzyloxy)carbonyl]-N-[(3R)-1-{N-[(benzyloxy)carbonyl]-L-leucyl}-4-oxo-3-pyrrolidinyl]-L-leucinamide	Cathepsin K	Ki (nM)	2	N/A	N/A	Details