title: Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).
abstract: Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogenTrypanosoma 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.
authors.affiliation: Northeastern University Department of Chemistry and Chemical Biology, 417 Egan Research Center, 360 Huntington Avenue, Boston, MA 02115, USA.
authors.forename: Emanuele
authors.initials: E
authors.lastname: Amata
authors.affiliation: Marine Biological Laboratory, Josephine Bay Paul Center for Comparative Molecular Biology and Evolution, 7 MBL Street, Woods Hole, MA 02543, USA.
authors.forename: Nicholas D
authors.initials: ND
authors.lastname: Bland
authors.affiliation: Marine Biological Laboratory, Josephine Bay Paul Center for Comparative Molecular Biology and Evolution, 7 MBL Street, Woods Hole, MA 02543, USA.
authors.forename: Robert K
authors.initials: RK
authors.lastname: Campbell
authors.affiliation: Northeastern University Department of Chemistry and Chemical Biology, 417 Egan Research Center, 360 Huntington Avenue, Boston, MA 02115, USA.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Pollastri
keywords: TbrPDEB1; Trypanosoma brucei; neglected tropical disease; phosphodiesterases