| Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition. | |
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MedLine Citation:
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PMID: 19435664 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Rita Capela; Rudi Oliveira; Lídia M Gonçalves; Ana Domingos; Jiri Gut; Philip J Rosenthal; Francisca Lopes; Rui Moreira |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't Date: 2009-05-03 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 19 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2009 Jun |
Date Detail:
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Created Date: 2009-05-29 Completed Date: 2009-08-21 Revised Date: 2013-04-12 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3229-32 Citation Subset: IM |
Affiliation:
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iMed.UL, Faculty of Pharmacy, University of Lisbon, Av Prof. Gama Pinto, 1649-003, Portugal. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals 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 | |
ID/Acronym/Agency:
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R56 AI035800-11A1/AI/NIAID NIH HHS |
| Chemical | |
Reg. No./Substance:
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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 |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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