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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: ioset jr. 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: ioset jr. 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
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
Papadopoulou MV, Bloomer WD, Lepesheva GI, Rosenzweig HS, Kaiser M, Aguilera-Venegas B, Wilkinson SR, Chatelain E, Ioset JR. Papadopoulou MV, et al. Among authors: ioset jr. J Med Chem. 2015 Feb 12;58(3):1307-19. doi: 10.1021/jm5015742. Epub 2015 Jan 23. J Med Chem. 2015. PMID: 25580906 Free PMC article.
48 results