Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587332 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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 headgroup of piclamilast, and found that these compounds exhibited weak inhibitory activity of TbrPDEB1.
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Authors
Jennifer L. Woodring, Nicholas D. Bland, Stefan O. Ochiana, Robert K. Campbell, Michael P. Pollastri,