Research Interests

• Design, synthesis and pharmacological study of new drugs and therapeutical tools.

• Physico-chemical parameters, e.g., ionization constants, lipophilicity.

• Analysis: assays, determination of purity and molecular structure of organic compounds.

• Biochemistry and pharmacology:

  • in vitro biological screening

  • evaluation of the in vivo biological activity

                Research Topics

• Drug Design

  • Ion channel and transporter modulators

    • ATP-sensitive K⁺ channels: activators and blockers

    • Allosteric modulators of AMPA receptors

    • Na⁺/H⁺ and Na⁺ / Ca⁺⁺ exchanger inhibitors 

    • SK channel modulators

  • Proteases inhibitors

  • Psychotropic drugs

  • Thromboxane A2 receptor antagonists

  • Thromboxane synthase inhibitors

  • Non steroïdal antiinflammatory drugs

• Biochemistry and pharmacology

• Cell cultures.

• Binding experiments.

• Ions fluxes.

• Tests on isolated organs.

• Diuresis, glycemia, convulsions.

• Behavioural studies.

                Service & Expertise

• Design of therapeutical compounds.

• Organic synthesis upon request.

• Analysis: Laboratory approved by the Belgian Ministry of Public Health  (ISO 17025 norm) :

  • Drug analysis and structure determination.

  • Elemental analyses (C, H, N, S).

  • ¹H-NMR, UV, and Infrared spectra.

  • Chromatrography (MPLC, HPLC and RP-HPLC techniques, TLC).

• Physico-Chemical parameters:

  • Ionization constants, such as pKa, by potentiometry and UV spectrophotometry.

  • lipophilicity, such as log P, by calculation, shake-flask and RP-HPLC.

                Equipement & Resources

• Elemental analyzer (C,H,N,S).

• UV spectrophotometers.

• FT-IR spectrophotometer.

• ¹H-NMR analyzer (500 MHz).

• HPLC equipments.

• Conventional equipment for organic synthesis.

                Publications

More than 250 articles in specialized international journals and several patents, for example :

• J. DELARGE, "Chemistry and Pharmacological Properties of the Pyridine-3 Sulfonylurea Derivatives Torasemide", Drug Research, 38, 144 (1988).

• J.-F. LIÉGEOIS et al., "New Pyridobenzodiazepine Derivative as potential Antipsychotics: Synthesis and Neurochemical Study", J. Med. Chem., 36, 2107 (1993).

• P. DE TULLIO et al., "3- and 4-substituted 4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potassium channel openers: synthesis, pharmacological evaluation, and structure-activity relationships", J. Med. Chem., 39, 937 (1996).

• L. POCHET et al., “Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of α-chymotrypsin: Significance of the “aromatic” nature of the novel ester-type coumarin for strong inhibitory activity”, J. Med. Chem. 39, 2579 (1996).

• B. PIROTTE et al., “3-alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis and pharmacological evaluation”, J. Med. Chem. 43, 1456 (2000).

• J.M. DOGNE et al., “Pharmacological characterization of N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time”, J. Pharmacol. Exp. Ther. 309, 498 (2004) 2004.
   

                Collaboration

Extensive national and international collaboration with other universities and pharmaceutical companies.