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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 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.

SUBMITTER: Amata E

PROVIDER: S-EPMC4426996 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature

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

Amata Emanuele E Bland Nicholas D ND Campbell Robert K RK Pollastri Michael P MP

Tetrahedron letters 20150501 21

Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen <i>Trypanosoma brucei</i>, 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. ...[more]

PMID: 25977593

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