Publication Date:
2022-05-25
Description:
Author Posting. © The Author(s), 2015. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Tetrahedron Letters 56 (2015): 2832-2835, doi:10.1016/j.tetlet.2015.04.061.
Description:
Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen
Trypanosoma brucei, which affects thousands every year and which is in need of new therapeutics.
Herein we report the synthesis and assessment of a series of pyrrolidine and pyrazolone derivatives of
human phosphodiesterase 4 (hPDE4) inhibitors for the assessment of their activity against the
trypanosomal phosphodiesterase TbrPDEB1. The synthesized compounds showed weak potency against
TbrPDEB1.
Description:
We acknowledge funding from the National Institutes of Health (R01AI082577).
Keywords:
Trypanosoma brucei
;
Phosphodiesterases
;
TbrPDEB1
;
Neglected tropical disease
Repository Name:
Woods Hole Open Access Server
Type:
Preprint
Format:
application/pdf
Format:
application/msword
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