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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2005-8-15
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pubmed:abstractText |
The increasing resistance of the malarial parasite to antimalarial drugs is a major contributor to the reemergence of the disease and increases the need for new drug targets. The two aspartic proteases, plasmepsins I and II, from Plasmodium falciparum have recently emerged as potential targets. In an effort to inhibit these hemoglobinases, a series of inhibitors encompassing a basic hydroxyethylamine transition state isostere as a central fragment were prepared. The synthesized compounds were varied in the P1' position and exhibited biological activities in the range of 31 to >2000 nM. To try to rationalize the results, molecular docking and 3D-QSAR analysis were used.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0968-0896
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5371-90
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16054370-Animals,
pubmed-meshheading:16054370-Antimalarials,
pubmed-meshheading:16054370-Aspartic Acid Endopeptidases,
pubmed-meshheading:16054370-Computer Simulation,
pubmed-meshheading:16054370-Models, Biological,
pubmed-meshheading:16054370-Models, Molecular,
pubmed-meshheading:16054370-Plasmodium falciparum,
pubmed-meshheading:16054370-Protease Inhibitors,
pubmed-meshheading:16054370-Protozoan Proteins,
pubmed-meshheading:16054370-Quantitative Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II.
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pubmed:affiliation |
Department of Medicinal Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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