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Discovery of Diaryl Ether Substituted Tetrahydrophthalazinones as TbrPDEB1 Inhibitors Following Structure-Based Virtual Screening.
de Heuvel E, Kooistra AJ, Edink E, van Klaveren S, Stuijt J, van der Meer T, Sadek P, Mabille D, Caljon G, Maes L, Siderius M, de Esch IJP, Sterk GJ, Leurs R. de Heuvel E, et al. Among authors: sterk gj. Front Chem. 2021 Jan 21;8:608030. doi: 10.3389/fchem.2020.608030. eCollection 2020. Front Chem. 2021. PMID: 33553105 Free PMC article.
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, Zorg S, Veerman J, Seebeck T, Sterk GJ, de Esch IJ, Leurs R. Orrling KM, et al. Among authors: sterk gj. J Med Chem. 2012 Oct 25;55(20):8745-56. doi: 10.1021/jm301059b. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22963052
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 KM, Jansen C, Cos P, Maes L, Chatelain E, Ioset JR, Edink EE, Tenor H, Seebeck T, de Esch I, Leurs R, Sterk GJ. Veerman J, et al. Among authors: sterk gj. Bioorg Med Chem. 2016 Apr 1;24(7):1573-81. doi: 10.1016/j.bmc.2016.02.032. Epub 2016 Feb 26. Bioorg Med Chem. 2016. PMID: 26935942
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R. Blaazer AR, et al. Among authors: sterk gj. J Med Chem. 2018 May 10;61(9):3870-3888. doi: 10.1021/acs.jmedchem.7b01670. Epub 2018 May 1. J Med Chem. 2018. PMID: 29672041 Free PMC article.
Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents.
Sijm M, Siciliano de Araújo J, Ramos Llorca A, Orrling K, Stiny L, Matheeussen A, Maes L, de Esch IJP, de Nazaré Correia Soeiro M, Sterk GJ, Leurs R. Sijm M, et al. Among authors: sterk gj. ChemMedChem. 2019 Sep 18;14(18):1662-1668. doi: 10.1002/cmdc.201900370. Epub 2019 Aug 23. ChemMedChem. 2019. PMID: 31319019 Free PMC article.
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).
de Heuvel E, Singh AK, Boronat P, Kooistra AJ, van der Meer T, Sadek P, Blaazer AR, Shaner NC, Bindels DS, Caljon G, Maes L, Sterk GJ, Siderius M, Oberholzer M, de Esch IJP, Brown DG, Leurs R. de Heuvel E, et al. Among authors: sterk gj. Bioorg Med Chem. 2019 Sep 15;27(18):4013-4029. doi: 10.1016/j.bmc.2019.06.026. Epub 2019 Jul 5. Bioorg Med Chem. 2019. PMID: 31378593 Free article.
Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.
De Araújo JS, da Silva PB, Batista MM, Peres RB, Cardoso-Santos C, Kalejaiye TD, Munday JC, De Heuvel E, Sterk GJ, Augustyns K, Salado IG, Matheeussen A, De Esch I, De Koning HP, Leurs R, Maes L, Soeiro MNC. De Araújo JS, et al. Among authors: sterk gj. J Antimicrob Chemother. 2020 Apr 1;75(4):958-967. doi: 10.1093/jac/dkz516. J Antimicrob Chemother. 2020. PMID: 31860098
47 results