Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1). Issue 21 (20th May 2015)

• Record Type: Journal Article
• Authors: Amata, Emanuele; Bland, Nicholas D.; Campbell, Robert K.; Pollastri, Michael P.
• Is Part Of: Tetrahedron letters. Volume 56:Issue 21(2015)
• Page Start: 2832
• Page End: 2835
• Publication Date: 2015-05-20
• Subjects: Trypanosoma brucei -- Phosphodiesterases -- TbrPDEB1 -- Neglected tropical disease; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2015.04.061
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: 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.