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Updated: Feb 13, 2026

Separation of Plasmodium falciparum Late Stage-infected Erythrocytes by Magnetic Means
Published on: March 2, 2013
Adamantane amine-linked chloroquinoline derivatives as chloroquine resistance modulating agents in Plasmodium
Opute M Yvette1, Sarel F Malan1, Dale Taylor2
1Pharmaceutical Chemistry, School of Pharmacy, University of the Western Cape, Private Bag X17, Bellville, South Africa.
Abstract:
Previously we have shown that pentacycloundecylamine-chloroquinoline (PCU-CQ) conjugates possess significant chemosensitizing abilities and can circumvent the resistance associated with chloroquine (CQ) resistant plasmodia. In order to further explore structurally related polycyclic compounds as reversed CQ agents we synthesized a series of eight aza-adamantanol (1-4) and adamantane-imine (5-8) CQ conjugates. All conjugates showed limited cytotoxicity against CHO cells (IC50 > 37 µM). Compounds 1, 2 and 5 were highly active (K1 IC50 < 100 nM) exhibiting a 3-4-fold increase in antiplasmodial activity against CQ resistant strain K1 compared to CQ. Reduced cross-resistance (resistance index, RI: 2-4.3) relative to CQ (RI = 38) was also observed for these compounds. Compound 1 which showed an 18-fold enhancement at retaining its activity against the K1 strain compared to CQ is a promising candidate to substitute CQ in P. falciparum resistant malaria.
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