## 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 curr
Synthesis of carbon-14-labelled pyronaridine tetraphosphate
✍ Scribed by Sang Hyun Park; Kannampalli Pradeep; Seung Ho Jang
- Publisher
- John Wiley and Sons
- Year
- 2007
- Tongue
- French
- Weight
- 153 KB
- Volume
- 50
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
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 for use in biodistribution studies and pharmacokinetic analysis. The application of microwave irradiation facilitated the use of high temperatures resulting in decreased reaction time and employed far less amount of the starting material when compared with the classical method. ^14^C‐PNDP (5) thus synthesized had a chemical purity of >99% as determined by high‐performance liquid chromatography (HPLC) and a radiochemical purity of >99% as determined by radio‐HPLC. Copyright © 2007 John Wiley & Sons, Ltd.
📜 SIMILAR VOLUMES
## Abstract A new antibacterial agent gemifloxacin was labelled with carbon‐14 for studies of pharmacokinetics and metabolism, the label was located in position 3 of the quinolone ring system. The overall radiochemical yield of the 14‐step synthesis, starting from [2‐^14^C]sodium acetate was 16.6%,
## Abstract Cytochrome P450 (CYP) enzymes are responsible for much of the phase I oxidative metabolism observed __in vivo__. Many important pharmaceutical compounds are metabolized by CYP. Co‐administration of a drug with another agent can alter the efficacy or the toxicity, especially in cases whe
## 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 t
## Abstract The syntheses of [^14^C] labelled antioxidants are described. We developed an efficient synthetic methodology to prepare a series of labelled amides with antioxidant activity, starting from [^14^C] KCN and alkyl or aryl halides. By a combination of nucleophilic displacement of halides b