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Synthesis of [2H]- and [13C]-labeled pyronaridine tetraphosphate—an antimalarial drug

✍ Scribed by Sang Hyun Park; Yeon Jun Jeong; Kannampalli Pradeep

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
228 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The increasing prevalence of strains of Plasmodium falciparum resistant to chloroquine and other antimalarial drugs, necessitates the need for developing novel antimalarial drugs with a potent pharmacological activity. Pyronaridine tetraphosphate (PNDP) is one such drug that is currently undergoing preclinical and clinical trials for use in a chemotherapy treatment of malaria. The present investigation was carried out with the objective of synthesizing carbon‐13 [^13^C]‐ and deuterium [^2^H]‐labeled PNDP for use in studying the ADME and pharmacokinetics of the drug. Here, we present a methodology to synthesize [^13^C]‐ and [^2^H]‐PNDP using a microwave irradiation technique as this method was found to be more advantageous than the classical method. The labeled compounds thus synthesized had a chemical purity of >99% as determined by HPLC and were also found to be relatively stable up to 3 months when stored under standard conditions. Further they also revealed satisfactory instrumental analysis data. Copyright © 2008 John Wiley & Sons, Ltd.

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