P. Raboisson

发表

Characterization of a dengue NS4B inhibitor originating from an HCV small molecule library

Peggy Geluykens, M. Van Loock, B. Devogelaere, 2017, Antiviral research.

In Vitro Activity and Preclinical Profile of TMC435350, a Potent Hepatitis C Virus Protease Inhibitor

L. Vrang, B. Samuelsson, Herman A de Kock, 2009, Antimicrobial Agents and Chemotherapy.

Running title: TMC435350, in vitro activity and pre-clinical profile

L. Vrang, B. Samuelsson, P. Wigerinck, 2009 .

The practice of medicinal chemistry

Didier Rognan, Camille Georges Wermuth, D. Rognan, 2015 .

Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor

L. Kwanten, J. McLellan, P. Rigaux, 2017, Nature Communications.

Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.

J. Vlach, F. Pauwels, E. Arnoult, 2016, Journal of medicinal chemistry.

1a/1b Subtype Profiling of Nonnucleoside Polymerase Inhibitors of Hepatitis C Virus

M. Cummings, B. Devogelaere, F. Pauwels, 2010, Journal of Virology.

Binding-Site Identification and Genotypic Profiling of Hepatitis C Virus Polymerase Inhibitors

F. Pauwels, O. Nyanguile, E. Cleiren, 2007, Journal of Virology.

Macrocycles: Under-Explored and Poorly Exploited Drug Class Despite the Proven Therapeutic Potential

P. Raboisson, 2015 .

Design, synthesis and structure-activity relationships of a series of 9-substituted adenine derivatives as selective phosphodiesterase type-4 inhibitors.

J. Bourguignon, J. Reimund, L. Désaubry, 2003, European journal of medicinal chemistry.

Anti-TNF-alpha properties of new 9-benzyladenine derivatives with selective phosphodiesterase-4- inhibiting properties.

J. Bourguignon, J. Reimund, C. Muller, 2001, Biochemical and biophysical research communications.

Efficient Synthesis of 8‐Substituted Pyrazolo[1,5‐a]‐1,3,5‐triazines by Regioselective Acylation.

J. Bourguignon, C. Lugnier, P. Raboisson, 2003 .

A general approach toward the synthesis of C-nucleoside pyrazolo[1,5-a]-1,3,5-triazines and their 3',5'-bisphosphate C-nucleotide analogues as the first reported in vivo stable P2Y(1)-receptor antagonists.

J. Bourguignon, J. Cazenave, C. Gachet, 2002, The Journal of organic chemistry.

Synthesis of 8‐Substituted Pyrazolo[1,5‐a]‐1,3,5‐triazine Derivatives by Palladium‐Catalyzed Cross‐Coupling Reactions.

P. Bernard, F. Popowycz, P. Raboisson, 2007 .

2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.

V. Pande, F. Pauwels, T. Jonckers, 2018, Journal of medicinal chemistry.

TMC647055, a Potent Nonnucleoside Hepatitis C Virus NS5B Polymerase Inhibitor with Cross-Genotypic Coverage

M. Cummings, R. Clayton, B. Devogelaere, 2012, Antimicrobial Agents and Chemotherapy.

Antiviral Activity and Mode of Action of TMC647078, a Novel Nucleoside Inhibitor of the Hepatitis C Virus NS5B Polymerase

B. Samuelsson, S. Eriksson, L. Leclercq, 2011, Antimicrobial Agents and Chemotherapy.

Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.

M. Cummings, B. Devogelaere, Lili Hu, 2012, Bioorganic & medicinal chemistry letters.

Discovery and Development of the HCV Protease Inhibitor TMC435

R. Verloes, P. Raboisson, K. Simmen, 2011 .

Evidence for microstructure in glow discharge hydrogenated amorphous Si-C alloys

R. Tsu, D. L. Williamson, A. Mahan, 1987 .

Regulation of gene transcription by thyroid hormone receptor β agonists in clinical development for the treatment of non-alcoholic steatohepatitis (NASH)

J. Deval, J. Symons, D. Misner, 2020, bioRxiv.

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.

L. Kwanten, J. McLellan, D. Roymans, 2020, Journal of medicinal chemistry.

Nucleotide prodrugs of 2'-deoxy-2'-spirooxetane ribonucleosides as novel inhibitors of the HCV NS5B polymerase.

B. Samuelsson, Lili Hu, L. Leclercq, 2014, Journal of medicinal chemistry.

Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.

M. Cummings, B. Devogelaere, Lili Hu, 2014, Journal of medicinal chemistry.

Influence of microstructure on the photoconductivity of glow discharge deposited amorphous SiC:H and amorphous SiGe:H alloys

R. Tsu, A. Mahan, P. Raboisson, 1987 .

On the differences between a-SiC:H films deposited with and without fluorine

D. L. Williamson, A. Mahan, P. Raboisson, 1985 .

Why the photoconductivity decreases in a-SiC:H and a-SiGe:H when the amount of alloying increases

R. Tsu, A. Mascarenhas, A. Mahan, 1988 .

Inhibition of platelet function by administration of MRS2179, a P2Y1 receptor antagonist.

J. Bourguignon, M. Freund, J. Cazenave, 2001, European journal of pharmacology.

Antiviral Properties and Mechanism of Action Studies of the Hepatitis B Virus Capsid Assembly Modulator JNJ-56136379

F. Pauwels, Karen Vergauwen, K. Vandyck, 2020, Antimicrobial Agents and Chemotherapy.

Novel antagonists acting at the P2Y(1) purinergic receptor: synthesis and conformational analysis using potentiometric and nuclear magnetic resonance titration techniques.

J. Bourguignon, J. Cazenave, C. Gachet, 2002, Journal of medicinal chemistry.

Discovery and development of simeprevir (TMC435), a HCV NS3/4A protease inhibitor.

B. Samuelsson, M. Cummings, Magnus Nilsson, 2014, Journal of medicinal chemistry.

Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.

L. Vrang, B. Samuelsson, Magnus Nilsson, 2012, Bioorganic & medicinal chemistry letters.

ALG-097111, a potent and selective SARS-CoV-2 3-chymotrypsin-like cysteine protease inhibitor exhibits in vivo efficacy in a Syrian Hamster model

A. Marchand, C. Liu, J. Neyts, 2021, bioRxiv.

Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).

Bing Huang, Ann Vos, Karen Vergauwen, 2018, Journal of medicinal chemistry.

The Substitutions L50F, E166A, and L167F in SARS-CoV-2 3CLpro Are Selected by a Protease Inhibitor In Vitro and Confer Resistance To Nirmatrelvir

P. Maes, A. Marchand, J. Neyts, 2022, bioRxiv.

Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors.

B. Samuelsson, Lili Hu, Magnus Nilsson, 2008, Bioorganic & medicinal chemistry letters.

Practical synthesis of (2'R)-2'-deoxy-2'-C-methyluridine by highly diastereoselective homogeneous hydrogenation.

T. Jonckers, R. Wechselberger, I. Houpis, 2011, The Journal of organic chemistry.

Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.

F. Pauwels, T. Jonckers, E. Arnoult, 2017, Journal of medicinal chemistry.

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity.

Tianbao Lu, M. Player, J. Marugan, 2006, Bioorganic & medicinal chemistry letters.

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo

D. Parks, Tianbao Lu, J. Marugan, 2006, Molecular Cancer Therapeutics.

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.

Maxwell D Cummings, Mark R Player, D. Parks, 2005, Bioorganic & medicinal chemistry letters.

In Vitro Resistance Profile of the Hepatitis C Virus NS3/4A Protease Inhibitor TMC435

L. Vrang, M. Cummings, Herman A de Kock, 2010, Antimicrobial Agents and Chemotherapy.

Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target.

Susanne Nyström, Maxwell D Cummings, Oliver Lenz, 2010, Angewandte Chemie.

1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.

M. Cummings, Lili Hu, F. Pauwels, 2009, Bioorganic & medicinal chemistry letters.

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.

Elizabeth Hamelink, L. Vrang, B. Samuelsson, 2008, Bioorganic & medicinal chemistry letters.

Structure-based design of a benzodiazepine scaffold yields a potent allosteric inhibitor of hepatitis C NS5B RNA polymerase.

Lili Hu, Maxwell D Cummings, M. Cummings, 2009, Journal of medicinal chemistry.

1,5-Benzodiazepines, a Novel Class of Hepatitis C Virus Polymerase Nonnucleoside Inhibitors

M. Cummings, F. Pauwels, O. Nyanguile, 2008, Antimicrobial Agents and Chemotherapy.

Monoaryl- and bisaryldihydroxytropolones as potent inhibitors of inositol monophosphatase.

J. Rondeau, P. Raboisson, F. Piriou, 1997, Journal of medicinal chemistry.

A general approach toward the synthesis of 8-acylamidopyrazolo[1,5-a]-1,3,5-triazines

J. Bourguignon, C. Lugnier, P. Raboisson, 2003 .

Efficient synthesis of 8-substituted pyrazolo[1,5-a]-1,3,5-triazines by regioselective acylation

J. Bourguignon, C. Lugnier, P. Raboisson, 2002 .

Practical Synthesis of Ethyl 3-Fluoro-1-pyrrole-2-carboxylate: A Key Fragment of a Potent Drug Candidate against Hepatitis B Virus

X. Pannecoucke, P. Jubault, T. Poisson, 2020, Organic Process Research & Development.

9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.

C. Wermuth, J. Bourguignon, L. Désaubry, 1997, Journal of medicinal chemistry.

2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.

B. Samuelsson, M. Cummings, Christophe Buyck, 2010, Journal of Medicinal Chemistry.

Efficient preparation of imidazo[1,2-b]pyridazines under Swern oxidative conditions

N. Peet, P. Raboisson, B. Mekonnen, 2003 .

Original articleNovel potent and selective αvβ3/αvβ5 integrin dual antagonists with reduced binding affinity for human serum albumin

Juan J. Marugan, B. Tomczuk, J. Marugan, 2006 .

Cyclic nucleotide phosphodiesterase type 4 inhibitors: evaluation of pyrazolo[1,5-a]-1,3,5-triazine ring system as an adenine bioisostere.

R. DesJarlais, J. Bourguignon, J. Reimund, 2003, European journal of medicinal chemistry.

Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.

O. Lenz, T. Verbinnen, S. Chakravarty, 2007, Bioorganic & medicinal chemistry letters.

From Oxetane to Thietane: Extending the Antiviral Spectrum of 2'-Spirocyclic Uridines by Substituting Oxygen with Sulfur.

J. Neefs, E. Jacoby, Peggy Geluykens, 2022, ACS medicinal chemistry letters.

Discovery of 1-((2R,4aR,6R,7R,7aR)-2-Isopropoxy-2-oxidodihydro-4H,6H-spiro[furo[3,2-d][1,3,2]dioxaphosphinine-7,2'-oxetan]-6-yl)pyrimidine-2,4(1H,3H)-dione (JNJ-54257099), a 3'-5'-Cyclic Phosphate Ester Prodrug of 2'-Deoxy-2'-Spirooxetane Uridine Triphosphate Useful for HCV Inhibition.

L. Leclercq, T. Jonckers, J. Snoeys, 2016, Journal of medicinal chemistry.

A small-molecule fusion inhibitor of influenza virus is orally active in mice

I. Wilson, Divita Garg, D. Roymans, 2019, Science.

Antiviral activity and mode of action of TMC 647078 , a novel 1 nucleoside inhibitor of the HCV NS 5 B polymerase 2 Running title : Characterization of HCV nucleoside inhibitor TMC 647078 3 4

B. Samuelsson, S. Eriksson, L. Leclercq, 2011 .

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.

Tianbao Lu, M. Player, J. Marugan, 2006, Bioorganic & medicinal chemistry letters.

Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.

F. Pauwels, T. Jonckers, E. Arnoult, 2018, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of novel HCV replication inhibitors

F. Pauwels, P. Raboisson, K. Simmen, 2017, Molecular Diversity.

Evaluation of SARS-CoV-2 3C-like protease inhibitors using self-assembled monolayer desorption ionization mass spectrometry

M. Scholle, C. Liu, J. Neyts, 2020, Antiviral Research.

Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor

J. McLellan, P. Rigaux, D. Roymans, 2017, Nature Communications.

Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties.

M. Cummings, B. Devogelaere, Lili Hu, 2012, Angewandte Chemie.

A pan-serotype dengue virus inhibitor targeting the NS3–NS4B interaction

Peggy Geluykens, R. Bartenschlager, A. Marchand, 2021, Nature.

Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists.

V. Pande, F. Pauwels, T. Jonckers, 2018, Bioorganic & medicinal chemistry letters.

Easy and general access to α,α-difluoromethylene phosphonothioic acids. A new class of compounds

P. Raboisson, S. Piettre, 1996 .

Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents.

Elizabeth Hamelink, L. Vrang, B. Samuelsson, 2010, Bioorganic & medicinal chemistry letters.

Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors.

L. Vrang, B. Samuelsson, Lili Hu, 2008, Bioorganic & medicinal chemistry letters.

Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series.

M. Cummings, Lili Hu, O. Nyanguile, 2012, Bioorganic & medicinal chemistry letters.

Identification of novel short chain 4-substituted indoles as potent αvβ3 antagonist using structure-based drug design

B. Tomczuk, R. DesJarlais, J. Marugan, 2007 .

Blocking NS3–NS4B interaction inhibits dengue virus in non-human primates

Gregory D. Gromowski, A. Barrett, D. Beasley, 2023, Nature.

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.

Maxwell D Cummings, D. Parks, Tianbao Lu, 2006, Bioorganic & medicinal chemistry letters.

Dual inhibition of SARS-CoV-2 and human rhinovirus with protease inhibitors in clinical development

M. Scholle, A. Marchand, J. Deval, 2021, Antiviral Research.

Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region.

Christophe Buyck, J. Grimes, J. Keown, 2019, Journal of medicinal chemistry.

Class A capsid assembly modulator RG7907 clears HBV-infected hepatocytes through core-dependent hepatocyte death and proliferation

S. Munck, T. Baumert, Nikky Corthout, 2023, Hepatology.