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Bioorg Med Chem Lett. 2008 Jan 15;18(2):624-8. Epub 2007 Nov 22.

Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.

Author information

1
Small Molecule Discovery Center, University of California, San Francisco, CA 94158, USA.

Abstract

A systematic study of P2 and P3 substitution in a series of vinyl sulfone cysteine protease inhibitors is described. The introduction of a methyl substituent in the P2 phenylalanine aryl ring had a favorable effect on protease inhibition and conferred modest selectivity for rhodesain over cruzain. Rhodesain selectivity could be enhanced further by combining these P2 modifications with certain P3 amide substituents.

PMID:
18055204
DOI:
10.1016/j.bmcl.2007.11.070
[Indexed for MEDLINE]

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