## Abstract Pyronaridine tetraphosphate is an antimalarial drug which is currently being widely investigated for use in the chemotherapy of malaria. We synthesized carbon‐14‐labelled pyronaridine tetraphosphate (^14^C‐PNDP, **5**) by a classical method and also by a microwave irradiation technique
Synthesis and biological evaluation of 131I-labelled pyronaridine
✍ Scribed by Sang Hyun Park; Hui Jeong Gwon; Kannampalli Pradeep
- Publisher
- John Wiley and Sons
- Year
- 2007
- Tongue
- French
- Weight
- 449 KB
- Volume
- 50
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
^131^I‐Labelled pyronaridine, an antimalarial drug was synthesized and evaluated for its stability and biodistribution in rabbits. We observed that there was >99% yield of the labelled compound as determined by HPLC and radio‐TLC in our study. Dynamic imaging studies in rabbits showed that ^131^I‐labelled pyronaridine was not concentrated in the thyroid for up to 30 min as that of Na^131^I. Biodistribution studies in the blood, liver, heart, spleen, kidney and lung of rats revealed that the maximum percentage of the injected dose (% ID) and the percentage of the injected dose per gram organ weight (% ID/g) of ^131^I‐labelled pyronaridine was found in the blood and liver when compared to the other organs even after 6 days of the drug administration. Results suggest that ^131^I‐labelled pyronaridine can be effectively used as an imaging agent to study the metabolism and mode of a response of pyronaridine. Copyright © 2007 John Wiley & Sons, Ltd.
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