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Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus.
Vendeville S, Tahri A, Hu L, Demin S, Cooymans L, Vos A, Kwanten L, Van den Berg J, Battles MB, McLellan JS, Koul A, Raboisson P, Roymans D, Jonckers THM. Vendeville S, et al. Among authors: raboisson p. J Med Chem. 2020 Aug 13;63(15):8046-8058. doi: 10.1021/acs.jmedchem.0c00226. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32407115
Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350.
Raboisson P, de Kock H, Rosenquist A, Nilsson M, Salvador-Oden L, Lin TI, Roue N, Ivanov V, Wähling H, Wickström K, Hamelink E, Edlund M, Vrang L, Vendeville S, Van de Vreken W, McGowan D, Tahri A, Hu L, Boutton C, Lenz O, Delouvroy F, Pille G, Surleraux D, Wigerinck P, Samuelsson B, Simmen K. Raboisson P, et al. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4853-8. doi: 10.1016/j.bmcl.2008.07.088. Epub 2008 Jul 24. Bioorg Med Chem Lett. 2008. PMID: 18678486
Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors.
Vendeville S, Nilsson M, de Kock H, Lin TI, Antonov D, Classon B, Ayesa S, Ivanov V, Johansson PO, Kahnberg P, Eneroth A, Wikstrom K, Vrang L, Edlund M, Lindström S, Van de Vreken W, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Van Dooren M, Kindermans N, Surleraux D, Wigerinck P, Rosenquist A, Samuelsson B, Simmen K, Raboisson P. Vendeville S, et al. Among authors: raboisson p. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6189-93. doi: 10.1016/j.bmcl.2008.10.004. Epub 2008 Oct 5. Bioorg Med Chem Lett. 2008. PMID: 18954982
1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.
McGowan D, Nyanguile O, Cummings MD, Vendeville S, Vandyck K, Van den Broeck W, Boutton CW, De Bondt H, Quirynen L, Amssoms K, Bonfanti JF, Last S, Rombauts K, Tahri A, Hu L, Delouvroy F, Vermeiren K, Vandercruyssen G, Van der Helm L, Cleiren E, Mostmans W, Lory P, Pille G, Van Emelen K, Fanning G, Pauwels F, Lin TI, Simmen K, Raboisson P. McGowan D, et al. Among authors: raboisson p. Bioorg Med Chem Lett. 2009 May 1;19(9):2492-6. doi: 10.1016/j.bmcl.2009.03.035. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19342234
1a/1b subtype profiling of nonnucleoside polymerase inhibitors of hepatitis C virus.
Nyanguile O, Devogelaere B, Vijgen L, Van den Broeck W, Pauwels F, Cummings MD, De Bondt HL, Vos AM, Berke JM, Lenz O, Vandercruyssen G, Vermeiren K, Mostmans W, Dehertogh P, Delouvroy F, Vendeville S, VanDyck K, Dockx K, Cleiren E, Raboisson P, Simmen KA, Fanning GC. Nyanguile O, et al. Among authors: raboisson p. J Virol. 2010 Mar;84(6):2923-34. doi: 10.1128/JVI.01980-09. Epub 2010 Jan 13. J Virol. 2010. PMID: 20071590 Free PMC article.
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.
Jonckers TH, Lin TI, Buyck C, Lachau-Durand S, Vandyck K, Van Hoof S, Vandekerckhove LA, Hu L, Berke JM, Vijgen L, Dillen LL, Cummings MD, de Kock H, Nilsson M, Sund C, Rydegård C, Samuelsson B, Rosenquist A, Fanning G, Van Emelen K, Simmen K, Raboisson P. Jonckers TH, et al. Among authors: raboisson p. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
Antiviral activity and mode of action of TMC647078, a novel nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Berke JM, Vijgen L, Lachau-Durand S, Powdrill MH, Rawe S, Sjuvarsson E, Eriksson S, Götte M, Fransen E, Dehertogh P, Van den Eynde C, Leclercq L, Jonckers TH, Raboisson P, Nilsson M, Samuelsson B, Rosenquist Å, Fanning GC, Lin TI. Berke JM, et al. Among authors: raboisson p. Antimicrob Agents Chemother. 2011 Aug;55(8):3812-20. doi: 10.1128/AAC.00214-11. Epub 2011 May 16. Antimicrob Agents Chemother. 2011. PMID: 21576430 Free PMC article.
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