Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi

Yoshinori Miyata; Hideaki Fujii; Yumiko Osa; Seiki Kobayashi; Tsutomu Takeuchi; Hiroshi Nagase

doi:10.1016/j.bmcl.2011.06.085

Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4710-2. doi: 10.1016/j.bmcl.2011.06.085. Epub 2011 Jun 25.

Authors

Yoshinori Miyata¹, Hideaki Fujii, Yumiko Osa, Seiki Kobayashi, Tsutomu Takeuchi, Hiroshi Nagase

Affiliation

¹ School of Pharmacy, Kitasato University, 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641, Japan.

PMID: 21764311
DOI: 10.1016/j.bmcl.2011.06.085

Abstract

We evaluated antimalarial and/or chloroquine-resistance reversing effects of five opioid receptor antagonists. Although none of the evaluated compounds showed antimalarial effects, some of them, especially the δ(1) receptor antagonist, 7-benzylidenenaltrexone (BNTX) exhibited potent chloroquine-resistance reversing effects in Plasmodium chabaudi.

MeSH terms

Antimalarials / chemistry
Antimalarials / pharmacology*
Benzylidene Compounds / chemistry
Benzylidene Compounds / pharmacology*
Chloroquine / pharmacology*
Drug Resistance / drug effects*
Molecular Structure
Naltrexone / analogs & derivatives*
Naltrexone / chemistry
Naltrexone / pharmacology
Parasitic Sensitivity Tests
Plasmodium chabaudi / drug effects*
Receptors, Opioid, mu / antagonists & inhibitors*
Stereoisomerism
Structure-Activity Relationship

Substances

Antimalarials
Benzylidene Compounds
Receptors, Opioid, mu
7-benzylidenenaltrexone
Naltrexone
Chloroquine