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Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Soeberdt M, Molenveld P, Storcken RP, Bouzanne des Mazery R, Sterk GJ, Autar R, Bolster MG, Wagner C, Aerts SN, van Holst FR, Wegert A, Tangherlini G, Frehland B, Schepmann D, Metze D, Lotts T, Knie U, Lin KY, Huang TY, Lai CC, Ständer S, Wünsch B, Abels C. Soeberdt M, et al. Among authors: sterk gj. J Med Chem. 2017 Mar 23;60(6):2526-2551. doi: 10.1021/acs.jmedchem.6b01868. Epub 2017 Mar 13. J Med Chem. 2017. PMID: 28218838
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Molenveld P, Bouzanne des Mazery R, Sterk GJ, Storcken RP, Autar R, van Oss B, van der Haas RN, Fröhlich R, Schepmann D, Wünsch B, Soeberdt M. Molenveld P, et al. Among authors: sterk gj. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5326-30. doi: 10.1016/j.bmcl.2015.09.040. Epub 2015 Sep 16. Bioorg Med Chem Lett. 2015. PMID: 26411794
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.
New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus.
Durcik M, Cotman AE, Toplak Ž, Možina Š, Skok Ž, Szili PE, Czikkely M, Maharramov E, Vu TH, Piras MV, Zidar N, Ilaš J, Zega A, Trontelj J, Pardo LA, Hughes D, Huseby D, Berruga-Fernández T, Cao S, Simoff I, Svensson R, Korol SV, Jin Z, Vicente F, Ramos MC, Mundy JEA, Maxwell A, Stevenson CEM, Lawson DM, Glinghammar B, Sjöström E, Bohlin M, Oreskär J, Alvér S, Janssen GV, Sterk GJ, Kikelj D, Pal C, Tomašič T, Peterlin Mašič L. Durcik M, et al. Among authors: sterk gj. J Med Chem. 2023 Mar 23;66(6):3968-3994. doi: 10.1021/acs.jmedchem.2c01905. Epub 2023 Mar 6. J Med Chem. 2023. PMID: 36877255 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
Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against Acinetobacter baumannii and Pseudomonas aeruginosa.
Cotman AE, Durcik M, Benedetto Tiz D, Fulgheri F, Secci D, Sterle M, Možina Š, Skok Ž, Zidar N, Zega A, Ilaš J, Peterlin Mašič L, Tomašič T, Hughes D, Huseby DL, Cao S, Garoff L, Berruga Fernández T, Giachou P, Crone L, Simoff I, Svensson R, Birnir B, Korol SV, Jin Z, Vicente F, Ramos MC, de la Cruz M, Glinghammar B, Lenhammar L, Henderson SR, Mundy JEA, Maxwell A, Stevenson CEM, Lawson DM, Janssen GV, Sterk GJ, Kikelj D. Cotman AE, et al. Among authors: sterk gj. J Med Chem. 2023 Jan 26;66(2):1380-1425. doi: 10.1021/acs.jmedchem.2c01597. Epub 2023 Jan 12. J Med Chem. 2023. PMID: 36634346 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.
47 results