Document Detail

Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.
MedLine Citation:
PMID:  19435664     Owner:  NLM     Status:  MEDLINE    
A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range.
Rita Capela; Rudi Oliveira; Lídia M Gonçalves; Ana Domingos; Jiri Gut; Philip J Rosenthal; Francisca Lopes; Rui Moreira
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2009-05-03
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2009-05-29     Completed Date:  2009-08-21     Revised Date:  2014-09-22    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3229-32     Citation Subset:  IM    
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MeSH Terms
Antimalarials / chemistry*,  pharmacology
Antiprotozoal Agents / chemistry,  pharmacology
Artemisinins / chemistry*,  pharmacology
Cysteine Endopeptidases / drug effects*
Dipeptides / chemistry,  pharmacology
Drug Design
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects
Structure-Activity Relationship
Sulfones / chemistry*,  pharmacology
Grant Support
Reg. No./Substance:
0/Antimalarials; 0/Antiprotozoal Agents; 0/Artemisinins; 0/Dipeptides; 0/Sulfones; 77-77-0/divinyl sulfone; EC 3.4.22.-/Cysteine Endopeptidases; EC 3.4.22.-/falcipain 2

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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