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Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Jun 07; Vol. 14 (11), pp. 2931-4. - Publication Year :
- 2004
-
Abstract
- Statine-based inhibitors of Plasmepsin II (PLMII) coupled with Primaquine have been designed using the 'double-drug' approach. The IC50 values for PLMII inhibition ranged from 0.59 to 400 nM and the best IC50 value for inhibition of Plasmodium falciparum growth in vitro was 0.4 microM, which represent a remarkable improvement compared to other statine-based PLMII inhibitors.
- Subjects :
- Amino Acids pharmacology
Animals
Antimalarials pharmacology
Chloroquine
Cross-Linking Reagents
Drug Design
Drug Resistance
Erythrocytes microbiology
Humans
Inhibitory Concentration 50
Plasmodium falciparum enzymology
Primaquine pharmacology
Protease Inhibitors pharmacology
Protozoan Proteins
Structure-Activity Relationship
Amino Acids chemistry
Antimalarials chemical synthesis
Aspartic Acid Endopeptidases antagonists & inhibitors
Plasmodium falciparum drug effects
Primaquine chemistry
Protease Inhibitors chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15125962
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.03.030