Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 11, Pages 2469-2472Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.014
Keywords
Schistosomiasis; Praziquantel; Supercritical fluid chromatography (SFC); Molecular probes; Anthelmintic
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Funding
- NIH NIAID grants [R56AI087807, 1R01AI087807-01A1]
- American Lebanese Syrian Associated Charities (ALSAC)
- St Jude Children's Research Hospital (SJCRH)
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Schistosomiasis is a highly prevalent neglected tropical disease caused by blood-dwelling helminths of the genus Schistosoma. Praziquantel (PZQ) is the only drug available widely for the treatment of this disease and is administered in racemic form, even though only the (R)-isomer has significant anthelmintic activity. Progress towards the development of a second generation of anthelmintics is hampered by a lack of understanding of the mechanism of action of PZQ. In this Letter, we report an efficient protocol for the small-scale separation of enantiomers of 2 (hydrolyzed PZQ) using supercritical fluid chromatography (SFC). The enantiopure 2 was then used to develop several molecular probes, which can potentially be used to help identify the protein target of PZQ and study its mode of action. (C) 2014 Elsevier Ltd. All rights reserved.
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