General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.

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Huang L, Ellman JA

General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2993-6.

PubMed ID

12270191 [ View in PubMed

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Abstract

A series of constrained ketone-based inhibitors has been developed that show low nanomolar Ki values. These ketone inhibitors showed promising activity towards cruzain, the cysteine protease implicated in Chagas' disease. This series of constrained inhibitors, which can be accessed quickly and efficiently using a solid-phase combinatorial strategy, should be applicable to other members of the cysteine protease class.

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)	2.3	N/A	N/A	Details