Antimalarial and antiplasmodial activities of norneolignans. Syntheses and SAR

Dorthe Mondrup Skytte; Simon Feldbaek Nielsen; Ming Chen; Lin Zhai; Carl Erik Olsen; Søren Brøgger Christensen

doi:10.1021/jm0508235

Antimalarial and antiplasmodial activities of norneolignans. Syntheses and SAR

J Med Chem. 2006 Jan 12;49(1):436-40. doi: 10.1021/jm0508235.

Authors

Dorthe Mondrup Skytte¹, Simon Feldbaek Nielsen, Ming Chen, Lin Zhai, Carl Erik Olsen, Søren Brøgger Christensen

Affiliation

¹ Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen Ø, Denmark.

PMID: 16392829
DOI: 10.1021/jm0508235

Abstract

A systematic change of the substituents and side chain of the norneolignan hinokiresinol afforded a 10 fold improvement of the IC(50) value toward inhibition of the growth of Plasmodium falciparum. The more potent compounds controlled the parasitemia in mice infected with Plasmodium berghei.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antimalarials / chemical synthesis*
Antimalarials / chemistry
Antimalarials / pharmacology*
Dose-Response Relationship, Drug
In Vitro Techniques
Lignans / chemical synthesis*
Lignans / chemistry
Lignans / pharmacology*
Malaria, Falciparum / drug therapy*
Malaria, Falciparum / parasitology
Mice
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium berghei / drug effects
Plasmodium falciparum / drug effects*
Plasmodium falciparum / growth & development
Structure-Activity Relationship

Substances

Antimalarials
Lignans