• 1855 Citations
  • 20 h-Index
19962020

Research output per year

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Research Output

Article

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

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
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155 Downloads (Pure)

3,6-Disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa

Frédérick, R., Robert, S., Masereel, B., Pochet, L., Pirotte, B., Charlier, C., De Ruyck, J. & Wouters, J., 1 Dec 2005, In : Journal of Medicinal Chemistry. 48, 24, p. 7592-7603 12 p.

Research output: Contribution to journalArticle

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

3D-QSAR, design, synthesis and characterization of trisubstituted harmine derivatives with in vitro antiproliferative properties

Meinguet, C., Bruyère, C., Frédérick, R., Mathieu, V., Vancraeynest, C., Pochet, L., Laloy, J., Mortier, J., Wolber, G., Kiss, R., Masereel, B. & Wouters, J., 13 Apr 2015, In : European Journal of Medicinal Chemistry. 94, p. 45-55 11 p., 7726.

Research output: Contribution to journalArticle

Open Access

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

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

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

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

Assessment of low plasma concentrations of apixaban in the periprocedural setting

Lessire, S., Dincq, A-S., Siriez, R., Pochet, L., Sennesael, A-L., Vornicu, O., Hardy, M., Deceuninck, O., Douxfils, J. & Mullier, F., 1 Aug 2020, In : International Journal of Laboratory Hematology. 42, 4, p. 394-402 9 p.

Research output: Contribution to journalArticle

File
82 Downloads (Pure)

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 electrophoretic mobility shift displacement assay for the assessment of weak drug-protein interactions

Farcaş, E., Hanson, J., Pochet, L. & Fillet, M., 30 Nov 2018, In : Analytica chimica acta. 1034, p. 214-222 9 p.

Research output: Contribution to journalArticle

Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors

Prevost, J. R. C., Kozlova, A., Es Saadi, B., Yildiz, E., Modaffari, S., Lambert, D. M., Pochet, L., Wouters, J., Dolušić, E. & Frédérick, R., 5 Dec 2018, In : Tetrahedron Letters. 59, 49, p. 4315-4319 5 p.

Research output: Contribution to journalArticle

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

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

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

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

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

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

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

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

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

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

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
188 Downloads (Pure)

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

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

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

Mechanism-based thrombin inhibitors: Design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative

Frédérick, R., Robert, S., Charlier, C., Wouters, J., Masereel, B. & Pochet, L., 26 Jul 2007, In : Journal of Medicinal Chemistry. 50, 15, p. 3645-3650 6 p.

Research output: Contribution to journalArticle

Modulators of the coagulation cascade: Focus and Recent Advances in Inhibitors of Tissue Factor, Factor VIIa and their complex

Frédérick, R., Pochet, L., Charlier, C. & Masereel, B., 2005, In : Current Medicinal Chemistry. 12, 4, p. 397-417 21 p.

Research output: Contribution to journalArticle

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

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

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

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

Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting D-alanyl-D-alanine ligase in bacterio

Ameryckx, A., Pochet, L., Wang, G., Yildiz, E., Saadi, B. E., Wouters, J., Van Bambeke, F. & Frédérick, R., 15 Aug 2020, In : European Journal of Medicinal Chemistry. 200, 112444.

Research output: Contribution to journalArticle

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

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

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

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

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
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Synthesis and pharmacological evaluation of a new targeted drug carrier system: beta-cyclodextrin coupled to oxytocin

Bertolla, C., Rolin, S., Evrard, B., Pochet, L. & Masereel, B., 2008, In : Bioorganic and medicinal chemistry letters. 18, 6, p. 1855-1858 4 p.

Research output: Contribution to journalArticle

Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties

Serra, S., Moineaux, L., Vancraeynest, C., Masereel, B., Wouters, J., Pochet, L. & Frédérick, R., 23 Jul 2014, In : European Journal of Medicinal Chemistry. 82, p. 96-105 10 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