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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6218-21. doi: 10.1016/j.bmcl.2009.08.098. Epub 2009 Sep 3.

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.

Author information

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

Abstract

We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 A) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such analogs bind the S2 and S3 subsites of the protease, effectively recapitulating important binding interactions present in more traditional peptide-based protease inhibitors and natural substrates.

PMID:
19773167
PMCID:
PMC3760505
DOI:
10.1016/j.bmcl.2009.08.098
[Indexed for MEDLINE]
Free PMC Article

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