Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)

Emanuele Amata; Nicholas D Bland; Robert K Campbell; Michael P Pollastri

doi:10.1016/j.tetlet.2015.04.061

Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1)

Tetrahedron Lett. 2015 May 20;56(21):2832-2835. doi: 10.1016/j.tetlet.2015.04.061.

Authors

Emanuele Amata¹, Nicholas D Bland², Robert K Campbell², Michael P Pollastri¹

Affiliations

¹ Northeastern University Department of Chemistry and Chemical Biology, 417 Egan Research Center, 360 Huntington Avenue, Boston, MA 02115, USA.
² Marine Biological Laboratory, Josephine Bay Paul Center for Comparative Molecular Biology and Evolution, 7 MBL Street, Woods Hole, MA 02543, USA.

Abstract

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.

Keywords: TbrPDEB1; Trypanosoma brucei; neglected tropical disease; phosphodiesterases.

Grants and funding

R01 AI082577/AI/NIAID NIH HHS/United States