Principales publications



Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
Donnier-Maréchal M., Carato P., Le Broc D., Furman C., Melnyk P.
Eur J Med Chem. 2015 92: 575-582.

Carboline- and phenothiazine-derivated heterocycles as potent sigma-1 ligands.
Donnier-Maréchal M, Larchanché P-E, Le Broc D, Furman C, Carato P, Melnyk P.
Eur J Med Chem. 2015 89: 198-206.

Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II).
Ettaoussi M, Peres B, Errazani A, Boutin JA, Caignard D-H, Delagrange P, Melnyk P, Berthelot P, Yous S.
Eur J Med Chem. 2015 90: 822-833.

6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands.
Larchanché P-E, Ultré V, Le Broc D, Ballandone C, Furman C, Dallemagne P, Melnyk P, Carato P.
Europ J Med. 2015 Chem accepted.

Efficient Synthesis of 1,3-Disubstituted-1,3-Dihydro-2H-imidazo[5,1-b]quinazolin-9-ones via an Intramolecular Mannich-Type Reaction.
Leclercq J., Driowya M., Flouquet N., Berthelot P., Lebegue N.
Synthesis 2015 47: 377-386.

Chloroquine and chloroquine related compounds as a model for the design of anti-Alzheimer compounds.
Melnyk P, Vingtdeux V, Burlet S, Eddarkaoui S, Grosjean M-E, Larchanché P-E, Hochart G, Sergheraert C, Estrella C, Barrier M, Poix V, Plancq P, Lannoo C, Hamdane M, Delacourte A, Verwaerde P, Buée L, Sergeant N
ACS Chem Neurosci. 2015 in press.

High affinity sigma-1 receptor agonist reduces clinical and pathological signs of experimental auto-immune encephalomyelitis.
Oxombre B, Lee-Chang C, Duhamel A, Toussaint M, Giroux M, Donnier-Maréchal M, Carato P, Lefranc D, Zephir H, Prin L, Melnyk P, Vermersch P.
British Journal of Pharmacol, 2015 accepted.

Thiocarbamate-linked polysulfonate-peptide conjugates as selective hepatocyte growth factor receptor binders.
Besret S, Vicogne J, Dhamani F, Fafeur V, Desmet R, Drobecq H, Romieu A, Melnyk P, Melnyk O.
Bioconjugate Chem. 2014 25(5): 1000-10.

Pharmacokinetic Evaluation of a Novel Benzopyridooxathiazepine Derivative as a Potential Anticancer Agent.
Bourdon F., Lecoeur M., Lebegue N., Gressier B., Luyckx M., Odou P., Dine T., Goossens, JF., Kambia N.
Pharmacology 2014 94: 170-178.

Hepatitis B Virus replication is blocked by a 2-hydroxyisoquinoline-1,3(2H,4H)-dione (HID) inhibitor of the viral ribonuclease H activity.
Cai CW, Lomonosova E, Moran EA, Cheng X, Patel KB, Bailly F, Cotelle P, Meyers MJ, Tavis JE.
Antivir Res. 2014 108:48-55. doi: 10.1016/j.antiviral.2014.05.007.

Synthesis, chiral resolution, absolute configuration assignment and pharmacological evaluation of a series of melatoninergic ligands.
Ettaoussi M, Pérès B, Jarry C, Pallage V, Nosjean O, Boutin JA, Gohier A, Mannoury la Cour C, Caignard DH, Delagrange P, Berthelot P, Yous S.
Med Chem Comm. 2014 5: 1590-1590

Recovery of brain biomarkers following PPAR agonist neuroprotective treatment before ischemic stroke.
Gelé P, Vingtdeux V, Drobecq H, Melnyk P, Ghestem A, Buée L, Sergeant N, Bordet R.
Proteome Science 2014 12: 24.

New Melatonin (MT1/MT2) Ligands: Design and Synthesis of (8,9-Dihydro-7H-furo[3,2-f]chromen-1-yl) Derivatives.
Landagaray E, Ettaoussi M, Leclerc V, Perez V, Nosjean O, Boutin JA, Caignard DH, Delagrange P, Berthelot P, Yous S.
Bioorg Med Chem 2014 22: 986-996.

Enantioseparation and thermodynamic study of naphthalene derivatives, new melatoninergic agonists, on coated amylose [tris(S)-1-phenylethylcarbamate] stationary phase. Transposition to preparative scale.
Landagaray E, Yous S, Vaccher C, Lipka E.
Biomedical Chromatography 2014 DOI: 10.1002/bmc.3332

Enhanced detection for determination of enantiomeric purity of novel agomelatine analogs by EKC using single and dual cyclodextrin systems.
Lipka E , Landagaray E , Ettaoussi M, Yous S , Vaccher C.
Electrophoresis 2014 35: 2785-2792.

Phenylthiocarbamate or N-carbothiophenylgroup chemistry in peptide synthesis or bioconjugation
Melnyk O, Ollivier N, Besret S, Melnyk P.
Bioconjugate Chem. 2014 25(4): 629-39.

Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases.
Melnyk P, Vermersch P, Carato P, Vanteghem-Oxombre B, Zephir H, Donnier-Maréchal M.
Brevet européen déposé le 16 juin 2014 sous le n° EP14305919.4.

Beta and gamma-carbolines derivatives for the treatment of neurodegenerative diseases.
Melnyk P, Carato P, Burlet S, Nguyen T-H, Verwaerde P, Sergeant N, Estrella C.
Demande PCT déposée le 27 juin 2014 sous le n° PCT/EP2014/063771.

Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as Human Immunodeficiency Virus Type 1 Integrase Inhibitors
Suchaud V, Bailly F, Lion C, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.
J Med Chem. 2014 57(11):4640-60. DOI: 10.1021/jm500109z.

Unexpected Heteroannelation and Chlorination of Benzothiadiazine Derivatives mediated by DDQ.
Verones V., Flouquet N., Farce A., Berthelot P., Lebegue N.
Synthesis 2014 46: 235-241.

Tau pathology modulates Pin1 post-translational modifications and may be relevant as biomarker.
Ando K, Sambo AV, Dourlen P, Bretteville A, Belarbi K, Vingtdeux V, Eddarkaoui S, Drobecq H, Ghestem A, Begard S, Demey-Thomas E, Melnyk P, Smet C, Lippens G, Maurage C-A, Caillet-Boudin M-L, Verdier Y, Vinh J, Landrieux I, Galas M-C, Blum D, Hamdane M, Sergeant N, Buée L.
Neurobiol Aging 2013 34 (3): 757-769. DOI: 10.1086/669517.

Antiproliferative and apoptotic effects of the oxidative dimerization product of methyl caffeate on human breast cancer cells.
Bailly F, Toillon RA, Tomavo O, Jouy N, Hondermarck H, Cotelle P.
Bioorg Med Chem. Lett 2013 23: 574-578. DOI: 10.1016/j.bmcl.2012.11.009

4-substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a novel class of HIV-1Integrase inhibitors
Billamboz M, Suchaud V, Bailly F, Lion C, Demeulemeester J, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.
ACS Med Chem Lett. 2013, DOI: 10.1021/ml400009t.

In vitro pharmacokinetic profile of a benzopyridooxathiazepine derivative using rat microsomes and hepatocytes: Identification of phases I and II metabolites.
Bourdon F, Lecoeur M, Verones V, Vaccher C, Lebegue N, Dine T, Kambia N, Goossens JF.
J Pharm Biomed Anal. 2013 80 : 69-78. DOI: 10.1016/j.jpba.2013. 02.022.

2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs), novel inhibitors of HIV integrase with a high barrier to resistance.
Desimmie BA, Demeulemeester J, Suchaud V, Taltynov O, Billamboz M, Lion C, Bailly F, Strelkov S, Debyser Z, Cotelle P, Christ F.
ACS Chem Biol. 2013 DOI: 10.1021/cb4000426.

Synthesis and Pharmacological Evaluation of a series of the Agomelatine Analogues as Melatonin MT1/MT2 Agonist and 5-HT2C Antagonist.
Ettaoussi M, Sabaouni A, Pérès B, Landagaray E, Nosjean O, Boutin JA, Caignard DH, Delagrange P, Berthelot P, Yous S.
Chem Med Chem. 2013 8: 1830-1845.

Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
Gonzalbez R, Mozulén S, Carbajo R, Melnyk P, Pineda-Lucena A
Bioorg Med Chem. 2013 21: 1944-1951. DOI: 10.1016/j.bmc.2013.01.033.

New radioligands for the description of MT1 and MT2 melatonin receptor molecular pharmacology.
Legros C, Matthey U, Grelak T, Pedragosa-Moreau S, Hasseler W, Yous S, Thomas E, Suzenet F, Folleas B, Lefoulon F, Berthelot P, Caignard DH, Guillaumet G, Delagrange P, Brayer JL, Nosjean O, Boutin JA
Int J Mol Sci. 2013 14(5): 8948-8962. DOI:10.3390/ijms14058948.

Exploring 6-(substituted sulfonyl)imidazopyridines as a potential scaffold for the design of 5-HT6 ligands.
Moas-Heloire V, Furman C, Melnyk P, Carato P.
Monatsch Chem. 2013 144(3): 425-435. DOI 10.1007/s00706-012-0893-3.

Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives.
Verones V, Flouquet N, Lecoeur M, Lemoine A, Farce A, Baldeyrou B, Mahieu C, Wattez N, Lansiaux A, Goossens J-F, Berthelot P, Lebegue N.
Eur J Med Chem. 2013 59: 39-47. DOI:10.1016/j.ejmech. 2012.10.051

γ-carbolines derivatives for the treatment of neurodegenerative diseases.
Melnyk P, Carato P, Burlet S, Nguyen T-H, Verwaerde P, Sergeant N, Estrella C.
(EP13305927.9, 2013 28th june)

β -carbolines derivatives for the treatment of neurodegenerative diseases
Melnyk P, Carato P, Burlet S, Nguyen T-H, Verwaerde P, Sergeant N, Estrella C.
(EP13305928.7, 2013 28th june)

Na-substituted carbolines derivatives for the treatment of neurodegenerative diseases.
Melnyk P, Carato P, Burlet S, Nguyen T-H, Verwaerde P, Sergeant N, Estrella C.
(EP13305929.5, 2013 28th june)

Methodology to access to dihydrodipyridoimidazole.
El Bousmaqui M, Donnier-Marechal M, Melnyk P, Carato P.
Heterocycles 2012 085 (9): 2135-2145. DOI: 10.3987/COM-12-12447.

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I)
Ettaoussi M, Sabaouni A, Rami M, Boutin JA, Delagrange P, Renard P, Spedding M, Caignard D-H, Berthelot P, Yous S.
Eur J Med Chem. 2012 49: 310-323. DOI: 10.1016/j.ejmech.2012.01.027.

Stereoselective synthesis of enantiopure N-protected-3-aryl piperazines from keto-esters.
Jida M, Laconde G, Soueidan OM, Lebegue N, Revelant G, Pelinski L, Agbossou-Niedercorn F, Deprez B, Deprez-Poulain R.
Tetrahedron Lett. 2012 53: 5215-5218. DOI: 10.1016/j.tetlet.2012.07.031.

Structural elucidation of degradation products of a benzopyridooxathiazepine under stress conditions using electrospray orbitrap mass spectrometry – Study of degradation kinetic.
Lecoeur M, Verones V, Vaccher C, Bonte JP, Lebegue N, Goossens J-F.
Eur J Pharm Sci. 2012 45 (5): 559-569. DOI: 10.1016/j.ejps.2011. 12.009 .

Effect of Oxime Ether Incorporation in Acyl Indole Derivatives on PPAR Subtype Selectivity.
Le Naour M, Leclerc V, Farce A, Caignard D-H, Hennuyer N, Staels B, Audinot-Bouchez V, Boutin JA, Lonchampt M, Dacquet C, Ktorza A, Berthelot P, Lebegue N.
Chem MedChem. 2012 7: 2179-2193. DOI: 10.1002/cmdc.201200316.

Analytical and Preparative Chiral Separation of beta-Carboline Derivatives, LDL Oxidation Inhibitors, Using HPLC and CE Methodologies: Determination of Enantiomeric Purity.
Lipka E, Yous S, Furman C, Carato P, Deghaye C, Bonte JP, Vaccher C.
Chromatographia. 2012 75 (7-8): 337-345. DOI: 10.1007/s10337-012-2194-8.

Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators.
Pirat C, Farce A, Lebegue N, Renault N, Furman C, Millet R, Yous S, Speca S, Berthelot P, Desreumaux P, Chavatte P.
J Med Chem. 2012 55 (9): 4027-4061. DOI: 10.1021/jm101360s .

Novel Conformationally Constrained Analogues of Agomelatine as New Melatoninergic Ligands.
Rami M, Landagaray E, Ettaoussi M, Boukhalfa K, Caignard DH, Delagrange P, Berthelot P, Yous S..
Molecules 2012 18: 154-166. 2012. DOI:10.3390/molecules18010154.

Development of a series of 3-hydroxyquinolin-2(1H)-ones as inhibitors of HIV-1 reverse transcriptase associated RNase H activity.
Suchaud V, Lion C, Tramontano E, Esposito F, Corona A, Christ F, Debyser Z, Cotelle P.
Bioorg Med Chem. Lett 2012 22: 3988-3992. DOI: 10.1016/j.bmcl.2012.04.096

Sulfate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d] imidazol-2-amine, preparation thereof and use of the same
Barrier M, Buée L, Burlet S, Delacourte A, Estrella C, Melnyk P, Sergeant N, Verwaerde P.
(EP12 306690.4 2012)

2-hydroxyisoquinoline-1,3(2h,4h)-diones and related compounds useful as HIV replication inhibitors
Bailly F, Billamboz M, Christ F, Cotelle P, Debyser Z, Lion C, Suchaud V.
(PCT Int. Appl. (2012), WO 2012085003 A1 20120628)

Composés de type spiroisoxazoline ayant une activité potentialisatrice de l’activité d’un antibiotique-composition et produits pharmaceutiques comprenant de tels composés.
Willand N, Brodin P, Agouridas-Dutot L, Deprez B, Baulard A.
(FR12/03549, 21st December 2012)

Kinetics and mechanism of racemisation of Tic-Hydantoins, potent sigma-1 agonists.
Cabordery A-C, Toussaint M, Azaroual N, Bonte J-P, Melnyk P, Vaccher C, Foulon C.
Tetrahedron Asym. 2011 22 (2): 125-133. DOI: 10.1016/j.tetasy.2011.01.015.

2-Hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.
Billamboz M, Bailly F, Lion C, Calmels C, Andréola ML, Witvrouw M, Christ F, Debyser Z, De Luca L, Chimirri A, Cotelle P.
Eur J Med Chem. 2011 46: 535-546. DOI: 10.1016/j.ejmech.2010.11.033.

Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function.
Billamboz M, Bailly F, Lion C, Touati N, Vezin H, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.
J Med Chem. 2011 54: 1812-1824. DOI: 10.1021/jm1014692.

3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1.
Cotelle P.
Expert Opin Ther Pat. 2011 21: 1799-1804. DOI: 10.1517/13543776.2011.624272.

Oleuropein and derivatives from olives as Tau aggregation inhibitors.
Daccache A, Lion C, Sibille N, Gerard M, Slomianny C, Lippens G, Cotelle P.
Neurochem Int. 58: 700-707. DOI: 10.1016/j.neuint. 2011. 02.010. IF (2011, 5-year) : 2,857 – 2,902

A novel and efficient one-pot synthesis of (aminophenyl)carbamic acid esters.
Garofalo A, Goossens L, Six P, Lebegue N, Depreux P.
Synthetic Commun. 2011 41: 2007- 2016 DOI: 10.1080/00397911.2010.494818.

Antioxydant activity of beta-carboline derivatives in the LDL oxidation model.
Hadjaz F, Besret S, Martin-Nizard F, Yous S, Dilly S, Lebegue N, Chavatte P, Duriez P, Berthelot P, Carato P.
Eur J Med Chem. 2011 46: 2575-2585. DOI: 10.1016/j.ejmech.2011.03.048.

Interactions of bexarotene (LGD1069, Targretin) with the coagulation system.
Hespel A, Mejdoubi-Charef N, Yous S, Courty J, Papy-Garcia D, Charef S.
Cancer Chemoth Pharm. 2011 201168: 847-54. DOI: 10.1007/s00280-010-1553-0.

Design and synthesis of naphthalenic derivatives as new ligands at the melatonin binding site MT3.
Leclerc V, Ettaoussi M, Rami M, Farce A, Boutin J-A, Delagrange P, Caignard D-H, Renard P, Berthelot P, Yous S.
Eur J Med Chem. 2011 46: 1622-1629. DOI: 10.1016/j.ejmech.2011.02.010

Step for the Synthesis of Metabolically More Stable Analogs of Amodiaquine.
Le Fur N, Hochart G, Larchanché P-E, Melnyk P (2011) Buchwald Reaction as the Key
Eur J Med Chem. 46 (7): 3052-3057. DOI: 10.1016/ j.ejmech.2011.04.047.

Preparation and Pharmacological Evaluation of A Novel Series of 2-(phenylthio) benzo[b]thiophenes As Selective MT2 Receptor Ligands.
Mésangeau C, Fraise M, Delagrange P, Caignard D-H, Boutin J-A, Berthelot P, Yous S.
Eur J Med Chem. 2011 46: 1835-1840. DOI: 10.1016/j.ejmech.2011.02.044.

Substituted 1,3-Benzothiazol-2(3H)-ones and Their N-Methyl Analogues by a Palladium Coupling Reaction.
Pirat C, Ultré V, Lebegue N, Berthelot P, Yous S, Carato P (2011) New Access to 5-
Synthesis 2011 24: 480-484. DOI: 10.1055/s-0030-1258377.

Separation of Tic-hydantoin enantiomers, potent sigma-1 agonist, by high performance liquid chromatography and capillary electrophoresis.
Cabordery A-C, Toussaint M, Bonte J-P, Melnyk P, Vaccher C, Foulon C.
J Chrom. 2010 A 1217 (24): 3871-5. DOI: 10.1016/j.chroma.2010.04.009.

Old and New Inhibitors of Quinone Reductase 2.
Ferry G, Hecht S, Berger S, Moulharat N, Coge G, Guillaumet G, Leclerc V, Yous S, Delagrange P, Boutin JA.
Chem Biol Interact. 2010 186 (2): 103-109. DOI: 10.1016/j.cbi.2010.04.006.

Efficient microwave-assisted two-step procedure for the synthesis of 1,3-disubstituted-imidazo[1,5-a]quinazolin-5-(4H)-ones.
Jankowski F, Verones V, Flouquet N, Carato P, Berthelot P, Lebegue N
Tetrahedron 2010 66: 128-133. DOI: 10.1016/j.tet.2009.11.025.

Optimized synthesis of potent anti-malarial aminoquinoline compounds: More convergent and easy access to analogs.
Le Fur N, Larchanché P-E, Melnyk P.
Heterocyclic Comm. 2011 16 (4-6): 235.239. DOI: 10.1515/HC.2010.011.

Evaluation of aldose reductase inhibition and docking studies of 6′-nitro and 6′,6”-dinitrorosmarinic acids.
Koukoulitsa C, Bailly F, Pegklidou K, Demopoulos VJ, Cotelle P.
Eur J Med Chem. 2010 45: 1663-1666. DOI:10.1016/j.ejmech.2009.12.007.

Dual cyclodextrin system in capillary electrophoresis for direct separation of the four stereoisomers of agonist and antagonist melatoninergic ligands.
Lipka E, Danel C, Yous S, Bonte JP, Vaccher C
Electrophoresis  2010 31 (9) : 1529-1532. DOI:10.1002/elps.200900661.

New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase – Discovery of a new polyhydroxylated antiviral agent.
Maurin C, Lion C, Bailly F, Touati N, Vezin H, Mbemba G, Mouscadet J-F, Debyser Z, Witvrouw M, Cotelle P (2010)
Bioorg Med Chem. 2010 18: 5194-5201.DOI: 10.1016/j.bmc.2010.05.059.

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands.
Mésangeau C, Pérès B, Descamps-François C, Chavatte P, Audinot V, Coumailleu S, Boutin JA, Delagrange P, Caignard DH, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
Bioorg Med Chem. 2010 18 (10) : 3426-3436. DOI: 10.1016/j.bmc.2009.03.023.

New synthesis of Tic-hydantoins sigma-1 ligands and pharmacological characterization on cocaine-induced stimulant effects.
Toussaint M, Debreu-Fontaine M-A, Maurice T, Melnyk P.
Med Chem. 2010 6(6): 355-73. DOI: 10.2174/157340610793563956.

Sigma-1 ligands : Tic-Hydantoin as a key pharmacophore.
Toussaint M, Mousset D, Foulon C, Jacquemard U, Vaccher C, Melnyk P.
Eur J Med Chem. 2010 45 (1): 256-263. DOI: 10.1016/j.ejmech.2009.10.004.

Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino [3,2-e]purine derivatives.
Verones V, Flouquet N, Farce A, Carato P, Leonce S, Pfeiffer B, Berthelot P, Lebegue N.
Eur J Med Chem. 2010 45(12): 5678-5684. DOI:10.1016/j.ejmech.2010.09.022.

Formulation and characterization of polyphenol-loaded lipid nanocapsules.
Barras A, Mezzetti A, Richard A, Lazzaroni S, Roux S, Melnyk P, Betbeder D, Dupont N.
Int J Pharm. 2009 379 (2): 270-277. DOI: 10.1016/j.ijpharm.2009.05.054.

The Facile Synthesis of 4-Alkoxycarbonylisoquinoline-1,3-diones and 5-Alkoxycarbonyl-2-benzazepine-1,3-diones via a Mild Alkaline Cyclization.
Billamboz M, Bailly F, Cotelle P.
J Heterocyclic Chem. 2009 46: 392-398. DOI: 10.1002/jhet.52.

Online H/D exchange liquid chromatography as a support for the mass spectrometric identification of the oxidation products of melatonin.
Collin F, Bonnefont-Rousselot D, Yous S, Marchetti C, Jore D, Gardès-Albert M.
J Mass Spectrom. 2009 44: 318-329. DOI: 10.1002/jms.1508.

New hexahydrodiazocinonaphthyridine triones as HIV-1 integrase inhibitors Merck: WO2008048538 A1.
Cotelle P.
Exp Opinion Therapeut Patents 2009 19: 87-93. DOI:10.1517/13543770802603577.

Synthesis of novel compounds with potential topoisomerase I inhibitors.
Delot M, Carato P, Furman C, Lemoine A, Lebegue N, Berthelot P, Yous S.
Synthesis 2009 22 : 3819-3822. DOI: 10.1055/s-0029-1217007.

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
Durieux S, Chanu A, Bochu C, Audinot V, Coumailleau S, Boutin J-A, Delagrange P, Caignard D-H, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
Bioorg Med Chem. 2009 17: 2963-2974. DOI: 10.1016/j.bmc.2009.03.023.

Benzopyridooxathiazepine derivatives as novel potent antimitotic agents.
Gallet S, Flouquet N, Carato P, Pfeiffer B, Renard P, Leonce S, Pierre A, Berthelot P, Lebegue N.
Bioorg Med Chem. 2009 17: 1132-1138. DOI: 10.1016/j.bmc.2008.12.039.

Rexinoid Bexarotene Modulates Triglyceride but not Cholesterol Metabolism via Gene-Specific Permissivity of the RXR/LXR Heterodimer in the Liver.
Lalloyer F, Pederson TA, Gross B, Lestavel S, Yous S, Vallez E, Gustafsson JA, Mandrup S, Fiévet C, Staels B, Tailleux A.
Arterioscl Throm Vas. 2009 29, 1488-1495. DOI: 10.1161/ATVBAHA.109.189506.

Replacement of 4’-hydroxy group of Amodiaquine and Amopyroquine by aromatic and aliphatic substituants: Synthesis and Antimalarial Activity.
Paunescu E, Susplugas S, Boll E, Varga R, Mouray E, Grosu I, Grellier P, Melnyk P.
Chem Med Chem. 2009 4 (4) : 549-561. DOI: 10.1002/cmdc.200800318.

S26948, a new specific peroxisome proliferator activated receptor gamma modulator improved in vivo hepatic insulin sensitivity in 48 h lipid infused rats.
Sohn K-AK, Cruciani-Guglielmacci C, Kassis N, Clément L, Ouali F, Caüzac M, Lebegue N, Berthelot P, Caignard D-H, Pégorier J-P, Renard P, Dacquet C, Ktorza A, Magnan C.
Eur J Pharmacol. 2009 608 : 104-111. DOI: 10.1016/j.ejphar.2009.02.033.

Tic hydantoin sigma-1 agonist: pharmacological characterization on cocaine-induced stimulant and appetitive effects.
Toussaint M, Delair B, Foulon C, Lempereur N, Vaccher C, Maurice T, Melnyk P.
Eur Neuropsychopharmacol. 2009 19 : 504-515. DOI:10.1016/j.euroneuro.2009.01.008.

Antioxidant activity of benzoxazolinonic and benzothiazolinonic derivatives in the LDL oxidation model.
Yekini I, Hammoudi F, Martin-Nizard F, Yous S, Lebegue N, Berthelot P, Carato P.
Bioorg Med Chem. 2009 17: 7823-7830. DOI : 10.1016/j.bmc.2009.09.016.

New Heterocycle compounds and uses thereof for the prevention or treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.
Melnyk P, Burlet S, Le Fur N, Delacourte A.
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