Synthesis of a bioprobe for elucidation of target molecule of spongean anti-malarial peroxides

Nobutoshi Murakami; Motoyuki Kawanishi; Sawako Itagaki; Toshihiro Horii; Motomasa Kobayashi

doi:10.1016/j.bmcl.2004.04.086

Synthesis of a bioprobe for elucidation of target molecule of spongean anti-malarial peroxides

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3513-6. doi: 10.1016/j.bmcl.2004.04.086.

Authors

Nobutoshi Murakami¹, Motoyuki Kawanishi, Sawako Itagaki, Toshihiro Horii, Motomasa Kobayashi

Affiliation

¹ Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.

PMID: 15177463
DOI: 10.1016/j.bmcl.2004.04.086

Abstract

The reactants of an anti-malarial peroxide having a 6-carbomethoxymethyl-3-methoxy-1,2-dioxane moiety treated with FeSO4 were analyzed. For mechanistic study of the anti-malarial peroxide, two biotinylated probes to elucidate the target molecules were designed and synthesized. The two synthesized probes showed potent anti-malarial activity, and one of them was proved to form an irreversible binding with protein in a model experiment.

Publication types

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

MeSH terms

Antimalarials / chemical synthesis*
Antimalarials / pharmacology
Biosensing Techniques*
Dioxanes / chemical synthesis
Dioxanes / pharmacology
Drug Design
Ferrous Compounds / chemistry
Ferrous Compounds / pharmacology
Humans
Models, Biological
Models, Chemical
Peroxides / chemical synthesis*
Peroxides / pharmacology
Protein Binding
Time Factors

Substances

Antimalarials
Dioxanes
Ferrous Compounds
Peroxides
ferrous sulfate