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

doi:10.1016/j.bmc.2016.02.032

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 Journal › Article › Academic › peer-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 language	English
Pages (from-to)	1573-1581
Journal	Bioorganic and Medicinal Chemistry
Volume	24
Issue number	7
DOIs	https://doi.org/10.1016/j.bmc.2016.02.032
Publication status	Published - 2016

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SDG 3 Good Health and Well-being

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10.1016/j.bmc.2016.02.032

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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. (2016). Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. Bioorganic and Medicinal Chemistry, 24(7), 1573-1581. https://doi.org/10.1016/j.bmc.2016.02.032

@article{989bcb494d16479398912395627fd6db,

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

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",

year = "2016",

doi = "10.1016/j.bmc.2016.02.032",

language = "English",

volume = "24",

pages = "1573--1581",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "7",

}

Veerman, J, van den Bergh, T, Orrling, KM, Jansen, CJW, Cos, P, Maes, L, Chatelain, E, Ioset, JR, Edink, ESE, Tenor, H, Seebeck, T, de Esch, IJP , Leurs, R & Sterk, GJ 2016, 'Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.', Bioorganic and Medicinal Chemistry, vol. 24, no. 7, pp. 1573-1581. https://doi.org/10.1016/j.bmc.2016.02.032

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

Research output: Contribution to Journal › Article › Academic › peer-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

Y1 - 2016

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

SN - 0968-0896

VL - 24

SP - 1573

EP - 1581

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 7

ER -

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

Abstract

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