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

…, SO Ochiana, RK Campbell, MP Pollastri

Index: Woodring, Jennifer L.; Bland, Nicholas D.; Ochiana, Stefan O.; Campbell, Robert K.; Pollastri, Michael P. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 21 p. 5971 - 5974

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Citation Number: 4

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 ...

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