1. Accueil
  2. Chémogénomique et Chimie Médicinale (CCM)
  3. Groupe Bihel / Schmitt
  4. Publications

Publications

2019

  • Fukuyama Cross-Coupling Approach to Isoprekinamycin: Discovery of the Highly Active and Bench-Stable Palladium Precatalyst POxAP 
    Tang S.-Q., Bricard J., Schmitt M., Bihel F.,*
    Organic Letters (2019) 21, 3, 844-848 (DOI : 10.1021/acs.orglett.9b00031)
    Post-print on HAL

  • On water N-arylation of oxetanylamines for the preparation of N-aryl-oxetanylamines; potentially useful aryl-amide isosteres
    Bollenbach M, Lecroq W, Wagner P, Fessard T, Schmitt M, Salomé C
    Chemical Communication (2019) 55, 1623-1626 (DOI : 10.1039/C8CC09110B)

  • Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model
    Bollenbach, M., Lugnier, C., Kremer, M., Salvat, E., Megat, S., Bihel, F., Bourguignon, J.-J., Barrot, M., and Schmitt
    European Journal of Medicinal Chemistry (2019) 177, 269–290. DOI: 10.1016/j.ejmech.2019.05.026
    Post-print on HAL

  • Mitochondria modulatory effects of new TSPO ligands in a cellular model of tauopathies.
    Grimm, A., Lejri, I., Hallé, F., Schmitt, M., Götz, J., Bihel, F., and Eckert, A.
    Journal of Neuroendocrinology (2019) DOI: 10.1111/jne.12796

  • TSPO ligands boost mitochondrial function and pregnenolone synthesis. 
    Lejri, I., Grimm, A., Hallé, F., Abarghaz, M., Klein, C., Maitre, M., Schmitt, M., Bourguignon, J.-J., Mensah-Nyagan, A.G., Bihel, F., Eckert A.
    Journal of Alzheimer’s Disease (2019) DOI: 10.3233/JAD-190127
  • Evolution of coumaroyl conjugate 3‐hydroxylases in land plants: Lignin biosynthesis and defense.
    Alber, A.V., Renault, H., Basilio Lopes, A., Bassard, J., Liu, Z., Ullmann, P., Lesot, A., Bihel, F., Schmitt, M., Werck‐Reichhart, D., Ehlting J.
    The Plant Journal (2019) DOI: 10.1111/tpj.14373

2018

  • Dioxygenation of Styrenes with Molecular Oxygen in Water.
    Tang, S.-Q., Wang, A.-P., Schmitt, M., Bihel, F.,*
    Tetrahedron Letters 59, 1465–1468
    https://doi.org/10.1016/j.tetlet.2018

  • Heteroarylguanidines as Allosteric Modulators of ASIC1a and ASIC3 Channels.
    Alijevic, O., Hammoud, H., Vaithia, A., Trendafilov, V., Bollenbach, M., Schmitt, M., Bihel, F.,* Kellenberger, S.* 
    ACS Chemical Neuroscience     9, 6, 1357-1365
    https://doi.org/10.1021/acschemneuro.7b00529

  • Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia.
    Hammoud, H., Elhabazi, K., Quillet, R., Bertin, I., Utard, V., Laboureyras, E., Bourguignon, J.-J., Bihel, F., Simonnet, G., Simonin, F.,* Schmitt, M.,*
    ACS Chemical Neuroscience 9, 11, 2599-2609
    https://doi.org/10.1021/acschemneuro.8b00099.03.009

  • Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation. 
    Bollenbach, M., Salvat, E., Daubeuf, F., Wagner, P., Yalcin, I., Humo, M., Letellier, B., Becker, L.J., Bihel, F., Bourguignon, J.-J., Villa, P., Obrecht, A., Frossard, N., Barrot, M., Schmitt, M.,* 
    European Journal of Medicinal Chemistry 23, 13676–13683
    https://doi.org/10.1016/j.ejmech.2018.01.049

  • Human erythrocytes release ATP by a novel pathway involving VDAC oligomerization independent of pannexin-1.
    Marginedas-Freixa, I., Alvarez, C.L., Moras, M., Leal Denis, M.F., Hattab, C., Halle, F., Bihel, F., Mouro-Chanteloup, I., Lefevre, S.D., Le Van Kim, C., Schwarzbaum, P.J., Ostuni, M.A. 
    Scientific Reports 8, 11384 https://doi.org/10.1038/s41598-018-29885-7

  • A bifunctional-biased mu-opioid agonist–neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects
    Drieu la Rochelle, A., Guillemyn, K., Dumitrascuta, M., Martin, C., Utard, V., Quillet, R., Schneider, S., Daubeuf, F., Willemse, T., Mampuys, P., Maes, B.U.W., Frossard, N., Bihel, F., Spetea, M., Simonin, F., Ballet, S. 
    PAIN 159, 9, 1705-1718
    https://doi.org/10.1097/j.pain.0000000000001262

  • Inhibition of neuronal FLT3 receptor tyrosine kinase alleviates peripheral neuropathic pain in mice.
    Rivat, C., Sar, C., Mechaly, I., Leyris, J.-P., Diouloufet, L., Sonrier, C., Philipson, Y., Lucas, O., Mallié, S., Jouvenel, A., Tassou, A., Haton, H., Venteo, S., Pin, J.-P., Trinquet, E., Charrier-Savournin, F., Mezghrani, A., Joly, W., Mion, J., Schmitt, M., Pattyn, A., Marmigère, F., Sokoloff, P., Carroll, P., Rognan, D., Valmier, J.,
    Nature Communications 9, 1042
    https://doi.org/10.1038/s41467-018-03496-2

  • Evidence for the involvement of TNF-α, IL-1β and IL-10 in the antinociceptive and anti-inflammatory effects of indole-3-guanylhydrazone hydrochloride, an aromatic aminoguanidine, in rodents.
    Sandes, S.M.S., Heimfarth, L., Brito, R.G., Santos, P.L., Gouveia, D.N., Carvalho, A.M.S., Quintans, J.S.S., da Silva-Júnior, E.F., de Aquino, T.M., França, P.H.B., de Araújo-Júnior, J.X., Albuquerque-Júnior, R.L.C., Zengin, G., Schmitt, M., Bourguignon, J.-J., Quintans-Júnior, L.J.,
    Chemico-Biological Interactions 286, 1–10.
    https://doi.org/10.1016/j.cbi.2018.02.026


2017

  • Efficient and mild Ullmann-type N-arylation of amides, carbamates, and azoles in water.
    Bollenbach, M., Aquino, P.G.V., de Araujo-Junior, J.X., Bourguignon, J.-J., Bihel, F., Salome, C., Wagner, P., Schmitt, M.*  
    Chemistry - A European Journal 23, 13676–13683. https://doi.org/10.1002/chem.201700832

  • RF313, an orally bioavailable neuropeptide FF receptor antagonist, opposes effects of RF-amide-related peptide-3 and opioid-induced hyperalgesia in rodents.
    Elhabazi, K., Humbert, J.-P., Bertin, I., Quillet, R., Utard, V., Schmitt, M., Bourguignon, J.-J., Laboureyras, E., Ben Boujema, M., Simonnet, G., Ancel, C., Simonneaux, V., Beltramo, M., Bucher, B., Sorg, T., Meziane, H., Schneider, E., Petit-Demoulière, B., Ilien, B., Bihel, F.,* Simonin, F.*  Neuropharmacology 118, 188–198. https://doi.org/10.1016/j.neuropharm.2017.03.012

  • Discovery of Imidazoquinazolinone Derivatives as TSPO Ligands Modulating Neurosteroidogenesis and Cellular Bioenergetics in Neuroblastoma Cells Expressing Amyloid Precursor Protein.
    Hallé, F., Lejri, I., Abarghaz, M., Grimm, A., Klein, C., Maitre, M., Schmitt, M., Bourguignon, J.-J., Mensah-Nyagan, A.G., Eckert, A.*, Bihel, F.*
    ChemistrySelect 2, 6452–6457. https://doi.org/10.1002/slct.201701565

  • The translocator protein ligand XBD173 improves clinical symptoms and neuropathological markers in the SJL/J mouse model of multiple sclerosis.
    Leva, G., Klein, C., Benyounes, J., Hallé, F., Bihel, F., Collongues, N., Seze, J.D., Mensah-Nyagan, A.-G., Patte-Mensah, C.
    Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease. https://doi.org/https://doi.org/10.1016/j.bbadis.2017.09.007

  • Development of a L-Tryptophan-Based Ligand for Regioselective Copper Catalyzed N 2 -Arylation of 1,2,3-Triazoles.
    Lopes, A.B., Wagner, P., Kümmerle, A.E., Bihel, F., Bourguignon, J.-J., Schmitt, M., Miranda, L.S.M.  ChemistrySelect 2, 6544–6548. https://doi.org/10.1002/slct.201701498

  • χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
    V    an der Poorten, O., Van Den Hauwe, R., Eiselt, E., Betti, C., Guillemyn, K., Chung, N.N., Hallé, F., Bihel, F., Schiller, P.W., Tourwé, D., Sarret, P., Gendron, L., Ballet, S.,
    ACS Medicinal Chemistry Letters 8, 1177–1182. https://doi.org/10.1021/acsmedchemlett.7b00347

  • A phenol-enriched cuticle is ancestral to lignin evolution in land plants
    Renault, H., Alber, A., Horst, N.A., Basilio Lopes, A., Fich, E.A., Kriegshauser, L., Wiedemann, G., Ullmann, P., Herrgott, L., Erhardt, M., Pineau, E., Ehlting, J., Schmitt, M., Rose, J.K.C., Reski, R., Werck-Reichhart, D., 
    Nature Communications 8, 14713. https://doi.org/10.1038/ncomms14713

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

  • Synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through regioselective 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

2011

  • New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam
    Bihel, F. J. J.;Justiniano, H.;Schmitt, M.;Hellal, M.;Ibrahim, M. A.;Lugnier, C. and Bourguignon, J. J.
    Bioorganic & Medicinal Chemistry Letters 2011, 21, 6567-6572

2010

  • Pharmacological characterization of the mouse NPFF2 receptor
    Talmont, F.;Mouledous, L.;Piedra-Garcia, L.;Schmitt, M.;Bihel, F.;Bourguignon, J. J.;Zajac, J. M. and Mollereau, C.
    Peptides 2010, 31, 215-220

  • Prefrontal cortex and reversion of atropine-induced disruption of the degraded contingency effect by antipsychotic agents and N-desmethylclozapine in rats
    Carnicella, S.;Mongeot, A.;Bourguignon, J. J. and Oberling, P.
    International Journal of Neuropsychopharmacology 2010, 13, 109-122

2009

  • The flavonoid dioclein is a selective inhibitor of cyclic nucleotide phosphodiesterase type 1 (PDE1) and a cGMP-dependent protein kinase (PKG) vasorelaxant in human vascular tissue
    Goncalves, R. L.;Lugnier, C.;Keravis, T.;Lopes, M. J.;Fantini, F. A.;Schmitt, M.;Cortes, S. F. and Lemos, V. S.
    European Journal of Pharmacology 2009, 620, 78-83

  • Evolution of a Novel Phenolic Pathway for Pollen Development
    Matsuno, M.;Compagnon, V.;Schoch, G. A.;Schmitt, M.;Debayle, D.;Bassard, J. E.;Pollet, B.;Hehn, A.;Heintz, D.;Ullmann, P.;Lapierre, C.;Bernier, F.;Ehlting, J. and Werck-Reichhart, D.
    Science 2009, 325, 1688-1692

  • Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH)
    Kummerle, A. E.;Vieira, M. M.;Schmitt, M.;Miranda, A. L. P.;Fraga, C. A. M.;Bourguignon, J. J. and Barreiro, E. J.
    Bioorganic & Medicinal Chemistry Letters 2009, 19, 4963-4966

  • Complexation with beta-cyclodextrin confers oral activity on the flavonoid dioclein
    Rezende, B. A.;Cortes, S. F.;De Sousa, F. B.;Lula, I. S.;Schmitt, M.;Sinisterra, R. D. and Lemos, V. S.
    International Journal of Pharmaceutics 2009, 367, 133-139

  • Rapid synthesis of imidazo[4,5-b]pyridine containing polycyclics by means of palladium-catalyzed amidation of 2-chloro-3-nitropyridine
    Salome, C.;Schmitt, M. and Bourguignon, J. J.
    Tetrahedron Letters 2009, 50, 3798-3800

2008

  • Cyclic nucleotide phosphodiesterase type 4 inhibitors: Evaluation of pyrazolo[1,5-a]-1,3,5-triazine ring system as an adenine bioisostere
    Raboisson, P.;Schultz, D.;Muller, C.;Reimund, J. M.;Pinna, G.;Mathieu, R.;Bernard, P.;Do, Q. T.;DesJarlais, R. L.;Justiano, H.;Lugnier, C. and Bourguignon, J. J.
    European Journal of Medicinal Chemistry 2008, 43, 816-829

  • 6-endo-dig Cyclization of heteroarylesters to alkynes promoted by Lewis acid catalyst in the presence of Bronsted acid
    Hellal, M.;Bourguignon, J. J. and Bihel, F. J. J.
    Tetrahedron Letters 2008, 49, 62-65

2007

  • Synthesis and reactivity of 2,3-dihydro-1H-2,3-benzodiazepine-1,4(5H)-dione
    Bihel, F. J. J.;Hellal, M. and Bourguignon, J. J.
    Synthesis-Stuttgart 2007, 24, 3791-3796

  • A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties
    Maillet, E. L.;Pellegrini, N.;Valant, C.;Bucher, B.;Hibert, M.;Bourguignon, J. J. and Galzi, J. L.
    Faseb Journal 2007, 21, 2124-2134

  • Neuropeptide FF and neuropeptide VF inhibit GABAergic neurotransmission in parvocellular neurons of the rat hypothalamic paraventricular nucleus
    Jhamandas, J. H.;Simonin, F.;Bourguignon, J. J. and Harris, K. H.
    American Journal of Physiology-Regulatory Integrative and Comparative Physiology 2007, 292, R1872-R1880

  • Synthesis of regiospecifically polysubstituted pyridazinones
    de Araujo-Junior, J. X.;Schmitt, M.;Antheaume, C. and Bourguignon, J. J.
    Tetrahedron Letters 2007, 48, 7817-7820

  • 2-Amino-6-iodo-4-tosyloxypyrimidine: a versatile key intermediate for regioselective functionalization of 2-aminopyrimidines in 4-and 6-positions
    Benderitter, P.;de Arajo, J. X.;Schmitt, M. and Bourguignon, J. J.
    Tetrahedron 2007, 63, 12465-12470

  • Isolation and NMR characterization of the indolomonoterpenoid alkaloids from Aspidosperma pyrifolium.
    de Araujo-Junior, J. X.; Antheaume, C.; Trindade, C.; Schmitt, M.; Bourguignon, J. J. and Santana AEG
    Phytochem. Rev.    , 2007, 6, 183-188

2006

  • Microwave-assisted cyclic amidine synthesis using TiCl4
    Hellal, M.;Bihel, F.;Mongeot, A. and Bourguignon, J. J.
    Organic & Biomolecular Chemistry 2006, 4, 3142-3146

  • Antiarrhythmogenic and antioxidant effect of the flavonoid dioclein in a model of cardiac ischemia/reperfusion
    Vianna, HR.; Cortes, SF.; Ferreira, AJ.; Capettini, LSA.; Schmitt, M.; Almeida, AP.; Massensini, AR. and Lemos, VS.
    Planta Med    ., 2006, 72 (4), 300-303

  • RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia
    Simonin, F.;Schmitt, M.;Laulin, J. P.;Laboureyras, E.;Jhamandas, J. H.;MacTavish, D.;Matifas, A.;Mollereau, C.;Laurent, P.;Parmentier, M.;Kieffer, B. L.;Bourguignon, J. J. and Simonnet, G.
    Proceedings of the National Academy of Sciences of the United States of America 2006, 103, 466-471

  • Sequential regio and chemoselective cross-coupling reactions by means of O-6-tri-isopropylsulfonate of 4-bromo-pyridazine 3,6-dione
    de Araujo-Junior, J. X.;Schmitt, M.;Benderitter, P. and Bourguignon, J. J.
    Tetrahedron Letters 2006, 47, 6125-6128

  • Use of 4-bromo pyridazine 3,6-dione for building 3-amino pyridazine libraries
    Schmitt, M.;de Araujo-Junior, J. X.;Oumouch, S. and Bourguignon, J. J.
    Molecular Diversity 2006, 10, 429-434

  • Stereoselective synthesis of 3 '-substituted 2 '-deoxy C-nucleoside pyrazolo[1,5-a]-1,3,5-triazines and their 5 '-phosphate nucleotides
    Mathieu, R.;Schmitt, M. and Bourguignon, J. J.
    Tetrahedron Letters 2006, 47, 5099-5103

  • Use of polyfunctionalized pyridazines as reactive species for building chemical diversity
    Bourguignon, J. J.;Oumouch, S. and Schmitt, M.
    Current Organic Chemistry 2006, 10, 277-295