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Research Output 1996 2019

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Article
2019
Chromogenics
Plasmas
Heparin
Assays
Low Molecular Weight Heparin
2018

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting D-alanine-D-alanine ligase in bacterio

Ameryckx, A., Thabault, L., Pochet, L., Leimanis, S., Poupaert, J., Wouters, J., Joris, B., Van Bambeke, F. & Frederick, R., 5 Nov 2018, In : European journal of medicinal chemistry / Chimica therapeutica. 159, 5, p. 324-338 15 p.

Research output: Contribution to journalArticle

Open Access
Anti-Infective Agents
Cytotoxicity
Cells
Peptidoglycan
Structure-Activity Relationship
18 Downloads (Pure)
File
Hemostasis
Viper Venoms
Thrombin Time
Coagulants
Partial Thromboplastin Time
Thromboxane B2
Liquid chromatography
Platelets
Tandem Mass Spectrometry
Liquid Chromatography

Effect of ABCB1 genetic polymorphisms on the transport of rivaroxaban in HEK293 recombinant cell lines

Sennesael, A. L., Panin, N., Vancraeynest, C., Pochet, L., Spinewine, A., Haufroid, V. & Elens, L., 1 Dec 2018, In : Scientific Reports. 8, 1, p. 10514 10514.

Research output: Contribution to journalArticle

HEK293 Cells
Genetic Polymorphisms
Single Nucleotide Polymorphism
Cell Line
Anticoagulants

Enhancing action of positive allosteric modulators through the design of dimeric compounds

Drapier, T., Geubelle, P., Bouckaert, C., Nielsen, L., Laulumaa, S., Goffin, E., Dilly, S., Francotte, P., Hanson, J., Pochet, L., Kastrup, J. S. & Pirotte, B., 28 Jun 2018, In : Journal of Medicinal Chemistry. 61, 12, p. 5279-5291 13 p.

Research output: Contribution to journalArticle

Benzothiadiazines
Ligands
Ethane
AMPA Receptors
HEK293 Cells
Nanoreactors
Capillary electrophoresis
Capillary Electrophoresis
Laminar flow
Assays
2017

An optimized dRVVT-based assay to estimate the intensity of anticoagulation in patients treated with direct oral anticoagulants

Sennesael, A-L., Exner, T., Chatelain, B., Lessire, S., Larock, A-S., Vancraeynest, C., Pochet, L., Dogné, J-M., Spinewine, A., Mullier, F. & Douxfils, J., 1 Sep 2017, In : Thrombosis Research. 157, p. 29-37 9 p.

Research output: Contribution to journalArticle

Prothrombin Time
Anticoagulants
Vitamin K
International Normalized Ratio
Tandem Mass Spectrometry

Capillary electrophoresis in the context of drug discovery

Farcaş, E., Pochet, L., Crommen, J., Servais, A. C. & Fillet, M., 10 Sep 2017, In : Journal of pharmaceutical and biomedical analysis. 144, p. 195-212 18 p.

Research output: Contribution to journalArticle

Capillary electrophoresis
Capillary Electrophoresis
Drug Discovery
Drug Industry
Drug Interactions

Discovery and assessment of water soluble coumarins as inhibitors of the coagulation contact pathway

Bouckaert, C., Zhu, S., Govers-Riemslag, J. W. P., Depoorter, M., Diamond, S. L. & Pochet, L., 1 Sep 2017, In : Thrombosis Research. 157, p. 126-133 8 p.

Research output: Contribution to journalArticle

Coumarins
Factor XIIa
Thrombosis
Water
Plasma Kallikrein

Partial filling affinity capillary electrophoresis as a useful tool for fragment-based drug discovery: A proof of concept on thrombin

Farcas, E., Bouckaert, C., Servais, A. C., Hanson, J., Pochet, L. & Fillet, M., 1 Sep 2017, In : Analytica chimica acta. 984, p. 211-222 12 p.

Research output: Contribution to journalArticle

Capillary electrophoresis
Capillary Electrophoresis
Drug Discovery
Thrombin
electrokinesis
Factor XIIa
Coumarins
Structure-Activity Relationship
Enzyme Precursors
Blood Coagulation
2015
62 Downloads (Pure)

29ièmes journées Franco-Belges de Pharmacochimie: Meeting report

Frédérick, R., Pochet, L., De Tullio, P. & Dufrasne, F., 17 Nov 2015, In : Pharmaceuticals. 8, 4, p. 758-777 20 p.

Research output: Contribution to journalArticle

Open Access
File
Open Access
Harmine
Quantitative Structure-Activity Relationship
Solubility
Derivatives
Cells
2014
Indoleamine-Pyrrole 2,3,-Dioxygenase
Derivatives
Scaffolds
Substitution reactions
Immunotherapy
2013

Determination of inhibitory potency of argatroban toward thrombin by electrophoretically mediated microanalysis

Pochet, L., Bouckaert, C., Servais, A-C., Farcas, E., Bettonville, V. & Fillet, M., 1 Jan 2013, In : Talanta. 116, p. 719-725 7 p.

Research output: Contribution to journalArticle

Thrombin
Assays
Chromogenic Compounds
Kinetics
Spectrophotometers
2012

Novel trisubstituted harmine derivatives with original in vitro anticancer activity

Frédérick, R., Bruyére, C., Vancraeynest, C., Reniers, J., Meinguet, C., Pochet, L., Backlund, A., Masereel, B., Kiss, R. & Wouters, J., 26 Jul 2012, In : Journal of Medicinal Chemistry. 55, 14, p. 6489-6501 13 p.

Research output: Contribution to journalArticle

Harmine
Carbolines
Neoplasms
Protein Synthesis Inhibitors
Cytostatic Agents
2011

Online magnetic bead based dynamic protein affinity selection coupled to LC-MS for the screening of acetylcholine binding protein ligands

Pochet, L., Heus, F., Jonker, N., Lingeman, H., Niessen, W. M. A., Kool, J. & Smit, A. B., 15 Jun 2011, In : Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences. 879, 20, p. 1781-1788 8 p.

Research output: Contribution to journalArticle

Acetylcholine
Carrier Proteins
Screening
Ligands
Proteins

Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators

Dolušić, E., Larrieu, P., Moineaux, L., Stroobant, V., Pilotte, L., Colau, D., Pochet, L., Van Den Eynde, B., Masereel, B., Wouters, J. & Frédérick, R., 11 Aug 2011, In : Journal of Medicinal Chemistry. 54, 15, p. 5320-5334 15 p.

Research output: Contribution to journalArticle

Tryptophan Oxygenase
Indoles
Immunologic Factors
Tryptophan
Indoleamine-Pyrrole 2,3,-Dioxygenase
2010

COU254, a specific 3-carboxamide-coumarin inhibitor of coagulation factor XII, does not protect mice from acute ischemic stroke

Kraft, P., Schwarz, T., Stoll, G., Kleinschnitz, C. & Pochet, L., 15 Feb 2010, In : Experimental and Translational Stroke Medicine. 2, 1

Research output: Contribution to journalArticle

Factor XII
Stroke
Middle Cerebral Artery Infarction
Thrombosis
Pharmacology

Deciphering the Mechanism of Carbonic Anhydrase Inhibition with Coumarins and Thiocoumarins

Maresca, A., Temperini, C., Pochet, L., Masereel, B., Scozzafava, A. & Supuran, C., 2010, In : Journal of Medicinal Chemistry. 53, p. 335-344 10 p.

Research output: Contribution to journalArticle

Coumarins
Carbonic Anhydrases
Protein Isoforms
Hydroxy Acids
Sulfonamides

Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation

Mortier, J., Frederick, R., Pochet, L., Wouters, J., Masereel, B., Ganeff, C., Remouchamps, C., Piette, J., Dejardin, E. & Talaga, P., 15 May 2010, In : Biochemical Pharmacology. 79, 10, p. 1462-1472 11 p.

Research output: Contribution to journalArticle

Isoquinolines
Phosphotransferases
Chemical activation
Enzyme Inhibitors
2009

Is thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs?

Robert, S., Ghiotto, J., Pirotte, B., David, J-L., Masereel, B., Pochet, L. & Dogné, J-M., 2009, In : Pharmacological Research. 59, 3, p. 160-166 7 p.

Research output: Contribution to journalArticle

2008

6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives in a new approach of the treatment of cancer cell invasion and metastasis

Kempen, I., Hemmer, M., Counerotte, S., de Tullio, P., Pirotte, B., Pochet, L., Foidart, J-M., Blacher, S., Noël, A. & Frankenne, F., 1 Dec 2008, In : European Journal of Medicinal Chemistry. 43, 12, p. 2735-2750 16 p.

Research output: Contribution to journalArticle

Benzopyrans
Carboxylic Acids
Esters
Cells
Neoplasm Metastasis

Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors

Robert, S., Bertolla, C., Masereel, B., Dogné, J-M. & Pochet, L., 2008, In : Journal of Medicinal Chemistry. 51, p. 3077-3081 5 p.

Research output: Contribution to journalArticle

2007
Benzopyrans
Thrombin
Derivatives
Factor Xa
Chymotrypsin

Synthesis, molecular modelling and enzymatic evaluation of (±) 3,5-diphenyl-2-thioxoimidazolidin-4-ones as new potential cyclooxygenase inhibitors

Gauthier, M-P., Michaux, C., Rolin, S., Vastersaegher, C., de Leval, X., Julémont, F., Pochet, L. & Masereel, B., 2006, In : Bioorganic and Medicinal Chemistry. 14, 4, p. 918-927 10 p.

Research output: Contribution to journalArticle

2005
Factor Xa
Thrombin
hydrazine
Coumarins
Chymotrypsin
Factor VIIa
Thromboplastin
Coagulation
Modulators
Inhibitory Concentration 50
2004

Coumarin and isocoumarin as serine protease inhibitors

Pochet, L., Frédérick, R. & Masereel, B., 1 Jan 2004, In : Current Pharmaceutical Design. 10, 30, p. 3781-3796 16 p.

Research output: Contribution to journalArticle

Isocoumarins
Serine Proteinase Inhibitors
Thrombin
Serine Proteases
Urokinase-Type Plasminogen Activator
2003

3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo

Kempen, I., Papapostolou, D., Thierry, N., Pochet, L., Counerotte, S., Masereel, B., Foidart, J-M., Reboud-Ravaux, M., Noel, A. & Pirotte, B., 2003, In : British Journal of Cancer. 88, p. 1111-1118 8 p.

Research output: Contribution to journalArticle

An overview of inhibitors of Na+/H+ exchanger

Masereel, B., Pochet, L. & Laeckmann, D., 2003, In : European Journal of Medicinal Chemistry. 38, p. 547-554 8 p.

Research output: Contribution to journalArticle

Investigation of the inhibition mechanism of coumarins on chymotrypsin by mass spectrometry

Pochet, L., Dieu, M., Frédérick, R., Murray, A-M., Kempen, I., Pirotte, B. & Masereel, B., 2003, In : Tetrahedron. 59, p. 4557-4561 5 p.

Research output: Contribution to journalArticle

2002

Structural approach of the mechanism of inhibition of α-chymotrypsin by coumarins

Wouters, J., Huygens, M., Pochet, L., Pirotte, B., Durant, F. & Masereel, B., 8 Apr 2002, In : Bioorganic and medicinal chemistry letters. 12, 7, p. 1109-1112 4 p.

Research output: Contribution to journalArticle

Coumarins
Chymotrypsin
2001
torsemide
Prostaglandin H2 Receptors Thromboxane A2
Thromboxane A2
Thromboxanes
Inhibitory Concentration 50
2000

Coumarinic derivatives as mechanism-based inhibitors of α-chymotrypsin and human leukocyte elastase

Pochet, L., Doucet, C., Dive, G., Wouters, J., Masereel, B., Reboud-Ravaux, M. & Pirotte, B., 1 Jun 2000, In : Bioorganic and Medicinal Chemistry. 8, 6, p. 1489-1501 13 p.

Research output: Contribution to journalArticle

Leukocyte Elastase
Chymotrypsin
Esters
Derivatives
Amides
1999

6-Substituted 2-Oxo-2H-1-benzopyran-3-carboxylic Acid as a Core Structure for Specific Inhibitors of Human Leukocyte Elastase

Doucet, C., Pochet, L., Thierry, N., Pirotte, B., Delarge, J. & Reboud-Ravaux, M., 1999, In : Journal of Medicinal Chemistry. 42, p. 4161-4171 11 p.

Research output: Contribution to journalArticle

Insulinotropic effect of new glibenclamide isosteres

Ouedraogo, R., Nguyen, QA., Antoine, M-H., Kane, C., Dunne, MJ., Pochet, L., Masereel, B. & Lebrun, P., 1999, In : Journal of Pharmacology and Experimental Therapeutics. 289, p. 625-631 7 p.

Research output: Contribution to journalArticle

Thromboxane A2 receptor antagonism in man and rat by a sulphonylcyanoguanidine (BM-144) and a sulphonylurea (BM-500)

Masereel, B., Damas, J., Fontaine, J., Lembège, M., Lacan, F., Nuhrich, A., Delarge, J., Pochet, L. & Dogné, J-M., 1999, In : Journal of Pharmacy and Pharmacology. 51, p. 695-701 7 p.

Research output: Contribution to journalArticle

1998

Design, synthesis, and anticonvulsant activity of 1-(pyrid-3- ylsulfonamido)-2-nitroethylenes

Masereel, B., Wouters, J., Pochet, L. & Lambert, D., 13 Aug 1998, In : Journal of Medicinal Chemistry. 41, 17, p. 3239-3244 6 p.

Research output: Contribution to journalArticle

Anticonvulsants
Phenytoin
Seizures
Strychnine
Picrotoxin
1997

Pharmacomodulation studies of torasemide led to original diuretic, neuroprotective, anticonvulsant and antithrombotic drugs.

Masereel, B., Dogné, J-M., Nuhrich, A., Varache-Lembège, M., Fontaine, J., Pochet, L., Somers, F., de Tullio, P., Pirotte, B. & Delarge, J., 1997, In : Journal de Pharmacie de Belgique. 52, p. 157-158 2 p.

Research output: Contribution to journalArticle

11 Downloads (Pure)

Synthesis and biological evaluation of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas

Masereel, B., Ouedraogo, R. B., Dogné, J-M., Antoine, M. H., De Tullio, P., Pirotte, B., Pochet, L., Delarge, J. & Lebrun, P. B., 1997, In : European Journal of Medicinal Chemistry. 32, 5, p. 453-456 4 p.

Research output: Contribution to journalArticle

Open Access
File
1996

Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: Significance of the «aromatic» nature of the novel ester-type coumarin for strong inhibitory activity.

Pochet, L., Doucet, C., Schynts, M., Thirry, N., Boggetto, N., Pirotte, B., Jiang, KY., Masereel, B., de Tullio, P., Delarge, J. & Reboud-Ravaux, M., 1996, In : Journal of Medicinal Chemistry. 1996, p. 2579-2585 7 p.

Research output: Contribution to journalArticle

175 Downloads (Pure)

First synthesis of 4-substituted-benzenesulfonylcyanoguanidines

Masereel, B., Lebrun, P., Dogné, J-M., de Tullio, P., Pirotte, B., Pochet, L., Diouf, O. & Delarge, J., 1996, In : Tetrahedron Letters. 37, p. 7253-7254 2 p.

Research output: Contribution to journalArticle

File