Publications and communications of Bernard Pirotte

Mvondo Mbala, J.-G., Thierry Mawete, D., Makiese, A., Kwiraviwe, L., Pangu, K., Nguimi, E., Cimanga Kanyanga, R., Pieters, L., Degotte, G., Frederich, M., Matondo, A., Van Pelt, N., Caljon, G., Pirotte, B., Mbala Mavinga, B., Bambi-Nyanguile, S.-M., & Mvondo, G. (24 December 2023). Synthesis and pharmacological evaluation of fluoro/chloro-substituted acetyl and benzoyl esters of quinine as antimalarial agents. Results in Chemistry, 7, 101284. doi:10.1016/j.rechem.2023.101284

Francotte, P., Bay, Y., Goffin, E., Colson, T., Lesenfants, C., Dorosz, J., Laulumaa, S., Fraikin, P., De Tullio, P., Beaufour, C., Botez, I., Pickering, D., Frydenvang, K., Danober, L., Skov Kristensen, A., Sandholm Kastrup, J., & Pirotte, B. (09 December 2023). Exploring thienothiadiazine dioxides as isosteric analogues of benzo-and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators. European Journal of Medicinal Chemistry, 264, 116036. doi:10.1016/j.ejmech.2023.116036

Arslan, D., Schoumacher, M., Dilly, S., Elmoualij, B., Zorzi, D., Quatresooz, P., Lambert, V., Noël, A., Pirotte, B., & De Tullio, P. (2023). Design, Synthesis, and Evaluation of Novel Pyruvate Dehydrogenase Kinase Inhibitors. Medicinal Chemistry, 19 (3), 276-296. doi:10.2174/1573406418666220819102627

Lesenfants, C., Goffin, E., Pirotte, B., Dammicco, S., & Francotte, P. (02 February 2022). Contribution to the synthesis of positive allosteric modulators of AMPA receptors for potential use in the early diagnosis of neurodegenerative diseases [Poster presentation]. CIRM Day, Liège, Belgium.

Abboud, D., Daly, A., Dupuis, N., Bahri, M. A., Inoue, A., Chevigné, A., Ectors, F., Plenevaux, A., Pirotte, B., Beckers, A., & Hanson, J. (21 September 2020). GPR101 drives growth hormone hypersecretion and gigantism in mice via constitutive activation of Gs and Gq/11. Nature Communications, 11 (1), 4752. doi:10.1038/s41467-020-18500-x

Etse, K. S., Comeron Lamela, L., Zaragoza, G., & Pirotte, B. (30 June 2020). Synthesis, crystal structure, Hirshfeld surface and interaction energies analysis of 5-methyl-1,3-bis(3-nitrobenzyl)pyrimidine-2,4(1H,3H)-dione. European Journal of Chemistry, 11/2, 91-99. doi:10.5155/eurjchem.11.2.91-99.1973

Matute Matute, A. F., Tabart, J., CHERAMY-BIEN, J.-P., Pirotte, B., Kevers, C., Auger, C., Schini-Kerth, V., Dommes, J., Defraigne, J.-O., & PINCEMAIL, J. (22 January 2020). Compared Phenolic Compound Contents of 22 Commercial Fruit and Vegetable Juices: Relationship to Ex-Vivo Vascular Reactivity and Potential In Vivo Projection. Antioxidants, 9 (2), 92. doi:10.3390/antiox9020092

Conlon, T., John-Schuster, G., Heide, D., Pfister, D., Lehmann, M., Hu, Y., Ertuz, Z., Lopez, M., Ansari, M., Strunz, M., Mayr, C., Cimineiri, C., Costa, R., Kohlhepp, M. S., Guillot, A., Günes, G., Jeridi, A., Funk, M., Beroshvili, G., ... Yildirim, A. Ö. (2020). Inhibition of LTβR-signalling activates Wnt-induced regeneration in lung. Nature. doi:10.1038/s41586-020-2882-8

Goffin, E., Jacques, N., Musumeci, L., Nchimi Longang, A., Oury, C., Lancellotti, P., & Pirotte, B. (2020). Synthesis of ticagrelor analogues belonging to 1,2,3-triazolo[4,5-d]pyrimidines and study of their antiplatelet and antibacterial activity. European Journal of Medicinal Chemistry, 208, 112767. doi:10.1016/j.ejmech.2020.112767

Degotte, G., Pirotte, B., Frederich, M., & Francotte, P. (22 November 2019). Total synthesis approach: development of new antimalarial compounds [Poster presentation]. MedChem 2019, Bruxelles, Belgium.

Etse, K. S., Zaragoza, G., & Pirotte, B. (30 September 2019). Crystal structure and Hirshfeld surface analysis of N-(2-(N-methylsulfamoyl)phenyl)formamide: Degradation product of 2-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide. European Journal of Chemistry, 10 (3), 189-194. doi:10.5155/eurjchem.10.3.189-194.1903

Degotte, G., Pirotte, B., Frederich, M., & Francotte, P. (05 September 2019). Pharmacomodulation of ellagic acid: a total synthesis approach [Poster presentation]. EFMC Young Medicinal Chemist, Athènes, Greece.

Oury, C., LANCELLOTTI, P., & Pirotte, B. (22 August 2019). Pyrimidine derivatives for prevention and treatment of bacterial infections.

Degotte, G., Halleux, A., Pirotte, B., Francotte, P., & Frederich, M. (May 2019). Design of new antimalarials inspired by ellagic acid through a total synthesis approach [Poster presentation]. Phytoday, Bruxelles, Belgium.

Lancellotti, P., Musumeci, L., Jacques, N., Servais, L., Goffin, E., Pirotte, B., & Oury, C. (2019). Antibacterial Activity of Ticagrelor in Conventional Antiplatelet Dosages Against Antibiotic-Resistant Gram-Positive Bacteria. JAMA Cardiology. doi:10.1001/jamacardio.2019.1189

Degotte, G., Halleux, A., Hans, A., Jansen, O., Ledoux, A., Desdemoustier, P., Pirotte, B., Francotte, P., & Frederich, M. (December 2018). Preparation of ellagic acid derivatives through a total synthesis approach to improve bioavailability [Poster presentation]. 1st CIRM Day, Liège, Belgium.

Degotte, G., Francotte, P., Frederich, M., Halleux, A., Hans, A., Jansen, O., Ledoux, A., Desdemoustier, P., & Pirotte, B. (November 2018). Pharmacomodulation of ellagic acid, a promising antiplasmodial agent, to improve its bioavailability [Poster presentation]. 30th International Symposium on the Chemistry of Natural Products and the 10th International Conference on Biodiversity, Athens, Greece.

Schnekenburger, M., Goffin, E., Lee, J.-Y., Jang, J. Y., Mazumder, A., Ji, S., Rogister, B., Bouider, N., Lefranc, F., Miklos, W., Mathieu, V., De Tullio, P., Kim, K.-W., Dicato, M., Berger, W., Han, B., Kiss, R., Pirotte, B., & Diederich, M. (08 June 2017). Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines. Journal of Medicinal Chemistry, 60 (11), 4714-4733. doi:10.1021/acs.jmedchem.7b00533

Abboud, D., Daly, A., Dupuis, N., Laschet, C., Geubelle, P., Pirotte, B., BECKERS, A., & Hanson, J. (May 2017). GPR101 orphan GPCR: a novel cause of growth hormone deregulation [Poster presentation]. 19th European Congress of Endocrinology, Lisbon, Portugal.

Drapier, T., Geubelle, P., Bouckaert, C., Goffin, E., Dilly, S., Hanson, J., Pochet, L., Kastrup, J. S., Francotte, P., & Pirotte, B. (26 May 2016). DESIGN OF HIGH-AFFINITY LIGANDS FOR THE BENZOTHIADIAZINE ALLOSTERIC BINDING SITE OF THE AMPA RECEPTORS [Poster presentation]. JFB 2016 : 30èmes Journées Franco-Belges de Pharmacochimie 25-27 May 2016 Amboise (France), Amboise, France.

Gilissen, J., Jouret, F., Pirotte, B., & Hanson, J. (2016). Insight into SUCNR1 (GPR91) structure and function. Pharmacology and Therapeutics. doi:10.1016/j.pharmthera.2016.01.008

Arslan, D., Pirotte, B., De Tullio, P., Charif, M. (Other coll.), Dilly, S. (Other coll.), Hansen, S. (Other coll.), LAMBERT, V. (Other coll.), Elmoualij, B. (Other coll.), & Noël, A. (Other coll.). (09 September 2014). AGE-RELATED MACULAR DEGENERATION (AMD): FROM METABOLOMICS APPROACH TO THE INHIBITION OF PDK AS A NEW THERAPEUTIC TARGET [Poster presentation]. XXIII International Symposium on Medicinal Chemistry (EFMC-ISMC 2014), Lisbonne, Portugal.

Renard, J.-F., Lecomte, F., Arslan, D., Hubert, P., & Pirotte, B. (May 2012). Evaluation de l'impact au niveau pharmacocinétique de modulations structurales de N-(pyrid-4-yl)alcanesulfonamides [Poster presentation]. 26èmes Journées franco-belges de pharmacochimie, Orléans, France.

Goffin, E., Lamoral-Theys, D., Tajeddine, N., De Tullio, P., Mondin, L., Lefranc, F., Gailly, P., ROGISTER, B., Kiss, R., & Pirotte, B. (2012). N-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis. European Journal of Medicinal Chemistry, 54, 834-44. doi:10.1016/j.ejmech.2012.06.050

Renard, J.-F., Lecomte, F., de Leval, X., Hubert, P., & Pirotte, B. (May 2011). Conception, synthèse et évaluation pharmacologique de N-(pyridin-4-yl)alcanesulfonamides en tant qu'inhibiteurs de cyclooxygénases [Poster presentation]. XVèmes Journées Franco-belges de pharmacochimie, Liège, Belgium.

Renard, J.-F., Lecomte, F., de Leval, X., Hubert, P., & Pirotte, B. (January 2011). Pyridine Derivatives of Nimesulide as New Promising Anti-inflammatory Agents [Poster presentation]. Giga Days, Liège, Belgium.

Renard, J.-F., Lecomte, F., de Leval, X., Hubert, P., & Pirotte, B. (21 May 2010). Nouveaux agents anti-inflammatoires en série N-(4-pyridyl)alcanesulfonamide [Paper presentation]. 24èmes JOURNEES FRANCO-BELGES DE PHARMACOCHIMIE, Woluwé-Saint-Lambert, Belgium.

Hemmer, M., Kempen, I., De Tullio, P., Frankenne, F., Lambert, V., Blacher, S., Bueb, J.-L., Foidart, J.-M., Noël, A., Tschirhart, E., & Pirotte, B. (2010). New Biological Investigations on 3-Bromophenyl 6-Acetoxymethyl-2-oxo-2H-1-Benzopyran-3-Carboxylate as Anti-angiogenic Agent. Drug Development Research, 71, 1-10. doi:10.1002/ddr.20364

Kempen, I., Hemmer, M., Counerotte, S., Pochet, L., De Tullio, P., Foidart, J.-M., Blacher, S., Noël, A., Frankenne, F., & Pirotte, B. (December 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. European Journal of Medicinal Chemistry, 43 (12), 2735-50. doi:10.1016/j.ejmech.2008.01.024

Hanson, J., Ghiotto, J., Neven, P., Kelley, L. P., Kinsella, B. T., Dogne, J. M., & Pirotte, B. (July 2006). Pharmacological evaluation of TP receptor antagonists characterized by differential activity on alpha and beta isoforms. Acta Pharmacologica Sinica, 27, 21.

Dogné, J.-M., Rolin, S., Petein, M., Tchana-Sato, V., Ghuysen, A., Lambermont, B., Hanson, J., Magis, D., Segers, P., Pirotte, B., Masereel, B., Drion, P., D'Orio, V., & Kolh, P. (2005). Characterization of an original model of myocardial infarction provoked by coronary artery thrombosis induced by ferric chloride in pig. Thrombosis Research, 116 (5), 431-442. doi:10.1016/j.thromres.2005.02.006

Kempen, I., Papapostolou, D., Thierry, N., Pochet, L., Counerotte, S., Masereel, B., Foidart, J.-M., Reboud-Ravaux, M., Noël, A., & Pirotte, B. (07 April 2003). 3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo. British Journal of Cancer, 88 (7), 1111-1118. doi:10.1038/sj.bjc.6600856

Dogné, J.-M., de Leval, X., Kolh, P., Sanna, V., Rolin, S., Michaux, C., Mauer, M., David, J.-L., Masereel, B., & Pirotte, B. (January 2003). Pharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function. Prostaglandins, Leukotrienes, and Essential Fatty Acids, 68 (1), 49-54. doi:10.1016/S0952-3278(02)00236-3

Cosgrove, K. E., Gonzalez, A. M., Lee, A. T., Barnes, P., Hussain, K., Aynsley-Green, A., Lindley, K. J., Pirotte, B., Lebrun, P., & Dunne, M. J. (2002). In vitro recovery of ATP-sensitive potassium channels in Beta-cells from patients with hyperinsulinism in infancy; effects of low temperature and BPDZ 154. Journal of Physiology, 544, 229.

Lee, A. T., Cosgrove, K. E., Barnes, P. D., Lindley, K. J., Aynsley-Green, A., De Tullio, P., Pirotte, B., Lebrun, P., & Dunne, M. J. (2002). BPDZ 154 is a potent activator of ATP-sensitive potassium channels in pancreatic b-cells. Endocrine abstracts 2002, 16.

Pochet, L., Doucet, C., Dive, G., Wouters, J., Masereel, B., Reboud-Ravaux, M., & Pirotte, B. (2000). Coumarinic derivatives as mechanism-based inhibitors of α-chymotrypsin and human leukocyte elastase. Bioorganic and Medicinal Chemistry, 8 (6), 1489-1501. doi:10.1016/S0968-0896(00)00071-7