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2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Embrechts W, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Pande V, Pille G, Amssoms K, Smyej I, Dhuyvetter D, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thone T, De Pooter D, Fanning G, Jonckers THM, Horton H, Raboisson P, McGowan D. Embrechts W, et al. J Med Chem. 2018 Jul 26;61(14):6236-6246. doi: 10.1021/acs.jmedchem.8b00643. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29965759
Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.
McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Scholliers A, Thoné T, Van Schoubroeck B, De Pooter D, Mostmans W, Khamlichi MD, Embrechts W, Dhuyvetter D, Smyej I, Arnoult E, Demin S, Borghys H, Fanning G, Vlach J, Raboisson P. McGowan D, et al. Among authors: embrechts w. J Med Chem. 2016 Sep 8;59(17):7936-49. doi: 10.1021/acs.jmedchem.6b00747. Epub 2016 Aug 23. J Med Chem. 2016. PMID: 27513093
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
McGowan DC, Herschke F, Pauwels F, Stoops B, Smyej I, Last S, Pieters S, Embrechts W, Khamlichi MD, Thoné T, Van Schoubroeck B, Mostmans W, Wuyts D, Verstappen D, Scholliers A, De Pooter D, Dhuyvetter D, Borghys H, Tuefferd M, Arnoult E, Hong J, Fanning G, Bollekens J, Urmaliya V, Teisman A, Horton H, Jonckers THM, Raboisson P. McGowan DC, et al. Among authors: embrechts w. J Med Chem. 2017 Jul 27;60(14):6137-6151. doi: 10.1021/acs.jmedchem.7b00365. Epub 2017 Jul 14. J Med Chem. 2017. PMID: 28671847
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.
Pieters S, McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Embrechts W, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thoné T, De Pooter D, Fanning G, Rosauro ML, Khamlichi MD, Houpis I, Arnoult E, Jonckers THM, Raboisson P. Pieters S, et al. Among authors: embrechts w. Bioorg Med Chem Lett. 2018 Feb 15;28(4):711-719. doi: 10.1016/j.bmcl.2018.01.014. Epub 2018 Jan 16. Bioorg Med Chem Lett. 2018. PMID: 29366653
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region.
McGowan DC, Balemans W, Embrechts W, Motte M, Keown JR, Buyck C, Corbera J, Funes M, Moreno L, Cooymans L, Tahri A, Eymard J, Stoops B, Strijbos R, Van den Berg J, Fodor E, Grimes JM, Koul A, Jonckers THM, Raboisson P, Guillemont J. McGowan DC, et al. Among authors: embrechts w. J Med Chem. 2019 Nov 14;62(21):9680-9690. doi: 10.1021/acs.jmedchem.9b01091. Epub 2019 Oct 30. J Med Chem. 2019. PMID: 31647875 Free PMC article.
Synthesis and biological evaluation of 1,2,4-triazinylphenylalkylthiazolecarboxylic acid esters as cytokine-inhibiting antedrugs with strong bronchodilating effects in an animal model of asthma.
Freyne EJ, Lacrampe JF, Deroose F, Boeckx GM, Willems M, Embrechts W, Coesemans E, Willems JJ, Fortin JM, Ligney Y, Dillen LL, Cools WF, Goossens J, Corens D, De Groot A, Van Wauwe JP. Freyne EJ, et al. Among authors: embrechts w. J Med Chem. 2005 Mar 24;48(6):2167-75. doi: 10.1021/jm049479m. J Med Chem. 2005. PMID: 15771459