Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

J. Veerman, T. van den Bergh, K.M. Orrling, C.J.W. Jansen, P. Cos, L. Maes, E. Chatelain, J.R. Ioset, E.S.E. Edink, H. Tenor, T. Seebeck, I.J.P. de Esch, R. Leurs, G.J. Sterk

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), also known as African sleeping sickness. Knock down of both enzymes leads to cell cycle arrest and is lethal to the parasite. Recently, we reported the phenylpyridazinone, NPD-001, with low nanomolar IC
Original languageEnglish
Pages (from-to)1573-1581
JournalBioorganic and Medicinal Chemistry
Volume24
Issue number7
DOIs
Publication statusPublished - 2016

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African Trypanosomiasis
Phosphodiesterase Inhibitors
Parasites
Trypanosoma brucei brucei
Phosphoric Diester Hydrolases
Cell Cycle Checkpoints
Life Cycle Stages
Life cycle
Cells
Enzymes
In Vitro Techniques
neodymium pyrocatechin disulfonate

Cite this

Veerman, J. ; van den Bergh, T. ; Orrling, K.M. ; Jansen, C.J.W. ; Cos, P. ; Maes, L. ; Chatelain, E. ; Ioset, J.R. ; Edink, E.S.E. ; Tenor, H. ; Seebeck, T. ; de Esch, I.J.P. ; Leurs, R. ; Sterk, G.J. / Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. In: Bioorganic and Medicinal Chemistry. 2016 ; Vol. 24, No. 7. pp. 1573-1581.
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abstract = "Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), also known as African sleeping sickness. Knock down of both enzymes leads to cell cycle arrest and is lethal to the parasite. Recently, we reported the phenylpyridazinone, NPD-001, with low nanomolar IC",
author = "J. Veerman and {van den Bergh}, T. and K.M. Orrling and C.J.W. Jansen and P. Cos and L. Maes and E. Chatelain and J.R. Ioset and E.S.E. Edink and H. Tenor and T. Seebeck and {de Esch}, I.J.P. and R. Leurs and G.J. Sterk",
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Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. / Veerman, J.; van den Bergh, T.; Orrling, K.M.; Jansen, C.J.W.; Cos, P.; Maes, L.; Chatelain, E.; Ioset, J.R.; Edink, E.S.E.; Tenor, H.; Seebeck, T.; de Esch, I.J.P.; Leurs, R.; Sterk, G.J.

In: Bioorganic and Medicinal Chemistry, Vol. 24, No. 7, 2016, p. 1573-1581.

Research output: Contribution to JournalArticleAcademicpeer-review

TY - JOUR

T1 - Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

AU - Veerman, J.

AU - van den Bergh, T.

AU - Orrling, K.M.

AU - Jansen, C.J.W.

AU - Cos, P.

AU - Maes, L.

AU - Chatelain, E.

AU - Ioset, J.R.

AU - Edink, E.S.E.

AU - Tenor, H.

AU - Seebeck, T.

AU - de Esch, I.J.P.

AU - Leurs, R.

AU - Sterk, G.J.

PY - 2016

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N2 - Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), also known as African sleeping sickness. Knock down of both enzymes leads to cell cycle arrest and is lethal to the parasite. Recently, we reported the phenylpyridazinone, NPD-001, with low nanomolar IC

AB - Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), also known as African sleeping sickness. Knock down of both enzymes leads to cell cycle arrest and is lethal to the parasite. Recently, we reported the phenylpyridazinone, NPD-001, with low nanomolar IC

U2 - 10.1016/j.bmc.2016.02.032

DO - 10.1016/j.bmc.2016.02.032

M3 - Article

VL - 24

SP - 1573

EP - 1581

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 7

ER -