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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