Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1) Journal Article


Authors: Woodring, Jennifer L.; Bland, Nicholas D.; Ochiana, Stefan O.; Campbell, Robert K.; Pollastri, Michael P.
Article Title: Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)
Abstract: Abstract Human African trypanosomiasis (HAT) is a parasitic neglected tropical disease that affects 10,000 patients each year. Current treatments are sub-optimal, and the disease is fatal if not treated. Herein, we report our continuing efforts to repurpose the human phosphodiesterase 4 (hPDE4) inhibitor piclamilast to target trypanosomal phosphodiesterase TbrPDEB1. We prepared a range of substituted heterocyclic replacements for the 4-amino-3,5-dichloro-pyridine head group of piclamilast, and found that these compounds exhibited weak inhibitory activity of TbrPDEB1.
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 23
Issue: 21
ISSN: 0960-894X
Publisher: Elsevier  
Date Published: 2013
Start Page: 5971
End Page: 5974
DOI/URL: