Publications


2017

  • RF313, an orally bioavailable NPFF receptor antagonist, opposes effects of RF-amide-related peptide-3 and opioid-induced hyperalgesia in rodents
    K Elhabazi, J-P Humbert, I Bertin, R Quillet, V Utard, M Schmitt, J-J Bourguignon, E Laboureyras, M Ben Boujema, G Simonnet, C Ancel, V Simonneaux, M Beltramo, B Bucher, T Sorg,, H Meziane, E Schneider,, B Petit-Demoulière,, B Ilien, F Bihel*, F Simonin*
    Neuropharmacol. 2017, accepted

2016

  • D-glucose : An efficient reducing agent for a Copper(II) mediated arylation of primary amines in water
    Bollenbach M, Wagner P, Aquino P, Bourguignon J-J, Bihel F, Salomé C, and Schmitt M
    ChemSusChem 2016, 9, 3244-3249

  • RF-Amide Neuropeptides And Their Receptors In Mammals : Pharmacological Properties, Drug Development And Main Physiological Functions.
    Quillet R, Ayachi S, Bihel F, Elhabazi K, Ilien B and Simonin F
    Pharmacol Ther.
    2016, 160, 84-132
  • Opioid adjuvant strategy : improving opioid effectiveness
    Bihel F
    Future Med. Chem.
    2016, 8, 339-354

  • Enantiopure synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through palladium-catalyzed intramolecular cyclization
    Hallé F., Van Der Poorten O., Doebelin C., Niederst M., Schneider S, Schmitt M., Ballet S., Bihel F.
    Tetrahedron Letters 2016, 57, 1547-1550
  • The effect of Neuropeptide FF in the amygdala kindling model
    Buffel I., Meurs A., Portelli J., Raedt R., De Herdt V., Poppe L., De Meulenaere V., Wadmann W., Bihel F., Schmitt M., Vonck K., Bourguignon J.J., Simonin F., Smolders I., Boon P.
    Acta Neurologica Scandinavica 2016, 134, 181-188

  • CMTX disorder and CamKinase
    Bihel F, Burkhard G, Fontes M
    Front. Cell. Neurosci. 2016, 10

  • Development of Dipeptidic hGPR54 Agonists
    C. Doebelin, I. Bertin, S. Schneider, M. Schmitt, J.-J. Bourguignon, C. Ancel, V. Simonneaux, F. Simonin, F. Bihel,
    ChemMedChem 2016, 11, 2147-2154.

  • TSPO ligands stimulate ZnPPIX transport and ROS accumulation leading to the inhibition of P. falciparum growth in human blood
    Marginedas-Freixa, I.;Hattab, C.;Bouyer, G.;Halle, F.;Chene, A.;Lefevre, S. D.;Cambot, M.;Cueff, A.;Schmitt, M.;Gamain, B.;Lacapere, J. J.;Egee, S.;Bihel, F.;Le Van Kim, C. and Ostuni, M. A.
    Scientific Reports 2016, 6, 33516

2015

  • Rapid and scalable synthesis of innovative unnatural α,β or γ-amino acids functionalized with tertiary amines on their side-chains.
    Schneider S, Ftouni H, Niu S, Schmitt M, Simonin F, Bihel F.
    Org Biomol Chem. 2015, 13(25), 7020-7026.

  • Development of a peptidomimetic antagonist of neuropeptide FF receptors for the prevention of opioid-induced hyperalgesia
    Bihel, F.; Humbert, JP.; Schneider, S.; Bertin, I.; Wagner, P.; Schmitt, M.; Laboureyras, E.; Petit-Demoulière, B.; Schneider, E.; Mollereau, C.; Simonnet, G.; Simonin, F. and Bourguignon J.J.
    ACS Chem Neuroscience
    2015, 6(3), 438-45
  • Effects of systematic N-terminus deletions and benzoylations of endogenous RF-amide peptides on NPFF1R, NPFF2R, GPR10, GPR54 and GPR103.
    Rouméas, L.; Humbert, J.-P.; Schneider, S.; Doebelin, C.; Bertin, I.; Schmitt, M.; Bourguignon, J.-J.; Simonin, F.; Bihel, F.
    Peptides 2015, 71, 156-161.

  • Neuropeptide FF receptors as novel targets for limbic seizure attenuation.
    Portelli J, Meurs A, Bihel F, Hammoud H, Schmitt M, De Kock J, Utard V, Humbert JP, Bertin I, Buffel I, Coppens J, Tourwe D, Maes V, De Prins A, Vanhaecke T, Massie A, Balasubramaniam A, Boon P, Bourguignon JJ, Simonin F, Smolders I.
    Neuropharmacology. 2015, 95, 415-423

  • Neuropeptide FF and prolactin releasing peptide decrease cortical excitability through activation of NPFF receptors
    Buffel, I.; Meurs, A.; Portelli, J.; Raedt, R.; De Herdt, V.; Sioncke, L.; Wadman, W.; Bihel, F.; Schmitt, M.; Vonck, K.; Bourguignon, J.-J.; Simonin, F.; Smolders, I. and Boon, P.
    Epilepsia 2015, 56(3), 489-98

  • The long-lasting love affair between the budding yeast Saccharomyces cerevisiae and the Epstein-Barr virus.
    Lista, M. J.; Voisset, C.; Contesse, M.-A.; Friocourt, G.; Daskalogianni, C.; Bihel, F.; Fåhraeus, R.; Blondel, M.
    Biotechnology Journal 2015, 16(11) 1670-1681

  • Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A.
    Blanc E, Wagner P, Plaisier F, Schmitt M, Durroux T, Bourguignon JJ, Partiseti M, Dupuis E, Bihel F.
    Anal Biochem. 2015, 484, 105-112
  • A Yeast/Drosophila screen to identify new compounds overcoming frataxin deficiency
    Seguin, A.; Monnier, V.; Palandri, A.; Bihel, F.; Rera, M.; Schmitt, M.; Camadro, J.-M.; Tricoire, H. and Lesuisse E.
    Oxidative Medicine and Cellular Longevity 2015, 565140

  • CMTX1 patients' cells present genomic instability corrected by CamKII inhibitors
    Mones, S.; Burkhardt, G.; Bordignon, B.; Altié, A.; Young, P.; Bihel, F.; Fraterno, M.; Peiretti, F.; Fontes, M.
    Orphanet Journal of Rare Diseases 2015, 10, 56


2014

  • Access to 4-Alkylaminopyridazine Derivatives via Nitrogen-Assisted Regioselective Pd-Catalyzed Reactions
    Blaise, E.;Kümmerle, A. E.;Hammoud, H.;de Araújo-Júnior, J. X.;Bihel, F.;Bourguignon, J.-J. and Schmitt, M.
    J Org Chem 2014, 79, 10311-10322
  • t-BuXPhos: a highly efficient ligand for Buchwald-Hartwig coupling in water.
    Wagner, P.; Bollenbach, M.; Doebelin, C.; Bihel, F.; Bourguignon, J.-J.; Salome, C.; Schmitt, M.
    Green Chem 2014, 16 (9), 4170-4178.

  • Structure-Activity Relationship Study around Guanabenz Identifies Two Derivatives Retaining Antiprion Activity but Having Lost alpha 2-Adrenergic Receptor Agonistic Activity
    Nguyen, P. H.;Hammoud, H.;Halliez, S.;Pang, Y. H.;Evrard, J.;Schmitt, M.;Oumata, N.;Bourguignon, J. J.;Sanyal, S.;Beringue, V.;Blondel, M.;Bihel, F. and Voisset, C.
    Acs Chemical Neuroscience 2014, 5, 1075-1082
  • Buchwald-Hartwig reactions in water using surfactants
    Salome, C.; Wagner, P.; Bollenbach, M.; Bihel, F.; Bourguignon, J. J.; Schmitt, M.
    Tetrahedron 2014, 70 (21), 3413-3421.

  • CamKII inhibitors reduce mitotic instability, connexon anomalies andp rogression of the in vivo behavioral phenotype in transgenic animals expressing a mutated Gjb1 gene.
    Mones, S.; Bordignon, B.; Peiretti, F.; Landrier, J. F.; Gess, B.; Bourguignon, J.-J.; Bihel, F.; Fontés, M.
    Frontiers in Neuroscience 2014, 8, 1-10.

  • Fully Regiocontrolled Polyarylation of Pyridine
    Doebelin, C.; Wagner, P.; Bihel, F.; Humbert, N.; Kenfack, C. A.; Mely, Y.; Bourguignon, J. J.; Schmitt, M.
    J Org Chem 2014, 79 (3), 908-918.


2013

  • The neuroprotector kynurenic acid increases neuronal cell survival through neprilysin induction
    Klein, C.; Patte-Mensah, C.; Taleb, O.; Bourguignon, J. J.; Schmitt, M.; Bihel, F.; Maitre, M.; Mensah-Nyagan, A. G.
    Neuropharmacology 2013, 70, 254-260.

  • N-Heteroarylation of Chiral alpha-Aminoesters by Means of Palladium-Catalyzed Buchwald-Hartwig Reaction.
    Hammoud, H.; Schmitt, M.; Blaise, E.; Bihel, F.; Bourguignon, J. J.
    J Org Chem 2013, 78 (16), 7930-7937.

  • Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors
    Elhabazi, K.; Humbert, J. P.; Bertin, I.; Schmitt, M.; Bihel, F.; Bourguignon, J. J.; Bucher, B.; Becker, J. A. J.; Sorg, T.; Meziane, H.; Petit-Demouliere, B.; Ilien, B.; Simonin, F.
    Neuropharmacology 2013, 75, 164-171.

  • Synthesis and Antiproliferative Effects of 5,6-Disubstituted Pyridazin-3(2H)-ones Designed as Conformationally Constrained Combretastatin A-4 Analogues
    Elagawany, M.; Schmitt, M.; Ghiaty, A.; El-Etrawy, A. S.; Ibrahim, M. A.; Bihel, F.; Sbardelotto, A. B.; Pessoa, C.; Nguyen, T. L.; Hamel, E.; Bourguignon, J. J.
    Anti-Cancer Agents inMed Chem 2013, 13 (7), 1133-1140.

  • Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists
    Doebelin, C.; Wagner, P.; Bertin, I.; Simonin, F.; Schmitt, M.; Bihel, F.; Bourguignon, J. J.
    Rsc Adv 2013, 3 (26), 10296-10300.

  • Nucleophilic Substitution of Azide Acting as a Pseudo Leaving Group: One-Step Synthesis of Various Aza Heterocycles
    Doebelin, C.; Schmitt, M.; Antheaume, C.; Bourguignon, J. J.; Bihel, F.
    J Org Chem 2013, 78 (22), 11335-11341.


2012

  • Direct Guanidinylation of Aryl and Heteroaryl Halides via Copper-Catalyzed Cross-Coupling Reaction
    Hammoud, H.; Schmitt, M.; Bihel, F.; Antheaume, C.; Bourguignon, J. J.
    J Org Chem 2012, 77 (1), 417-423

  • Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors
    Gealageas, R.; Schneider, S.; Humbert, J. P.; Bertin, I.; Schmitt, M.; Laboureyras, E.; Dugave, C.; Mollereau, C.; Simonnet, G.; Bourguignon, J. J.; Simonin, F.; Bihel, F.
    Bioorg Med Chem Lett 2012, 22 (24), 7471-7474

  • Involvement of neuropeptide FF receptors in neuroadaptive responses to acute and chronic opiate treatments
    Elhabazi, K.; Trigo, J. M.; Mollereau, C.; Mouledous, L.; Zajac, J. M.; Bihel, F.; Schmitt, M.; Bourguignon, J. J.; Meziane, H.; Petit-demouliere, B.; Bockel, F.; Maldonado, R.; Simonin, F.
    Brit J Pharmacol 2012, 165 (2), 424-435.

  • Palladium-Catalyzed Synthesis of Substituted Pyrido[2,3-d]pyridazines at Positions 5 and 8
    Ibrahim, M. A.; Blaise, E.; Lozach, O.; Szalata, C.; Schmitt, M.; El-Etrawy, A. A. S.; Elagawany, M.; El-Feky, S. A.; Abdel-Samii, Z. K.; Meijer, L.; Bourguignon, J. J.; Bihel, F.
    Synthesis-Stuttgart 2012, 44 (20), 3216-3224.

  • 1-Phenyl-3H-2,3-benzodiazepin-4(5H)-one
    Ballo, D.; Bihel, F.; Doubia, M. L.; Essassi, E. M.; Ng, S. W.
    Acta Crystallographica Section E 2012, E68, o2443.

  • Toward versatile methods leading to highly functionnalized imidazo [1,2-a]pyridines
    Basilio-Lopes, A; De Aquino Mendonca, T; Mongeot, A; Bourguignon, JJ; Schmitt, M
    Tetrahedron Lett 2012, 53(21), 2583-2587

  • Design, Synthesis, and Pharmacological Evaluation of N-Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase-4 Inhibitors
    Kummerle, AE; Schmitt, M; Cardozo, SVS; Lugnier, C; Villa, P; Lopes, AB; Romeiro, NC; Justiniano, H; Martins, MA; Fraga, CAM; Bourguignon, JJ;  Barreiro, E.
    J Med Chem 2012, 55(17), 7525-7545

  • Protein-protein and protein-membrane associations in the lignin pathway
    Bassard, JE; Richert, L; Geerinck, J; Renault, H; Duval, F; Ullmann, P; Schmitt, M; Meyer, E; Mutterer, J; Boerjan, W; Werck, D.
    Plant Cell 2012, 24(11), 4465-4482

  • Xanthurenic acid binds to neuronal G-protein-coupled receptors that secondarily activate cationic channels in the cell line NCB-20
    Taleb, O; Maammar, M; Brumaru, D; Bourguignon, JJ; Schmitt, M; Klein, C; Kemmel, V; Maitre, M; Mensah-Nyagan, AG
    PLoS One 2012, 7(11), e48553

  • Synthesis, sigma(1), sigma(2)-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes
    Riganas, S; Papanastasiou, I; Foscolos, GB; Tsotinis, A; Bourguignon, JJ; Serin, G; Mirjolet, JF; Dimas, K; Kourafalos, VN; Eleutheriades, A; Moutsos, VI; Khan, H; Georgakopoulou, S; Zaniou, A; Prassa, M; Theodoropoulou, M; Pondiki, St; Vamvakides, A.
    Bioorg  Med Chem 2012, 20(10), 3323-3331

  • Novel access to 1,4-benzodiazepin-2-ones via the Buchwald reaction and application to the synthesis of novel heterocyclics
    Salome, C; Schmitt, M; Bourguignon, JJ.
    Tetrahedron Lett 2012, 53(9), 1033-1035

  • Disease progression in MRL/lpr lupus-prone mice is reduced by NCS 613, a specific cyclic nucleotide phosphodiesterase type 4 (PDE4) inhibitor
    Keravis, T; Monneaux, F; Yougbare, I; Gazin, L; Bourguignon, JJ; Muller, S; Lugnier, C.
    PLoS One 2012, 7(1), e28899