Jean-michel Brunel
bruneljm
yahoo.fr
+33 (0)4.86.13.68.30
Main Interests
Our project teams gather chemists cooperating with and biologists who work on novel target discovery and validation. Our mission is to design and prepare specific inhibitors and/or ligands modulating the effects of proteins in vitro first and in animal model ultimately. In this context, these compounds serve first as pharmacological probe to validate therapeutic approaches and then as drug prototypes. Our know-how is a combination of academic experience. It spans from medicinal chemistry, asymmetric catalysis and organometallic chemistry to achieve our goals in the organoselective synthesis of biologically active molecules. We foster close ties with industrial teams and academic researchers, especially with structural biologists and molecular modellers. We are also open to any collaboration where medicinal chemistry, screening can unlatch new drug research and accelerate the translation of new therapeutic concept into drug discovery.
Selected publications
- 1) "A New and Efficient Method for the Resolution of 1,1'-binaphthalene-2,2'-diol" Brunel, J. M.; Buono, G. J. Org. Chem. 1993, 58, 7313-7314.
- 2) "Highly Enantioselective Oxidation of Sulfides Mediated by a Chiral Titanium Complex" Brunel, J. M.; Diter, P.; Duetsch, M.; Kagan, H. B. J. Org. Chem. 1995, 60, 8086-8088.
- 3) "Catalytic Asymmetric Oxidation of Sulfides with High Enantioselectivities" Brunel, J. M.; Kagan, H. B. Synlett 1996, 404-406.
- 4) "Totally Stereoselective P-O to P-C Migration Rearrangement : Application to the Synthesis of New Chiral o-Hydroxyaryl Phosphine Oxides" Legrand, O. ; Brunel, J. M.; Constantieux, T. ; Buono, G. Chem. Eur. J. 1998, 4, 1061-1067.
- 5) "New Ring Expansion Reaction of Chiral Diazaphospholidine Oxides via a Totally Stereospecific P-N to P-Csp2 Migration Rearrangement" Legrand, O. ; Brunel, J. M. ; Buono, G. Angew. Chem., Int. Ed. Engl. 1999, 38, 1479-1483.
- 6) "Highly Efficient Phosphapalladacyclic Catalysts for the Hydroarylation of Norbornene" Brunel, J. M. ; Heumann, A. ; Buono, G. Angew. Chem., Int. Ed. Engl. 2000, 39, 1946-1949.
- 7) "Highly Efficient Phosphazene Base-Catalyzed Michael Addition of b-Ketoesters in Water" Bensa, D. ; Brunel, J. M. ; G. ; Buono, G. ; Rodriguez, J. Synlett 2001, 715-717.
8) " Recent Advances in the Synthesis of Spermine and Spermidine Analogs of the Shark Aminosterol Squalamine "Brunel, J. M. ; Letourneux, Y. Eur : J. Org. Chem. 2003, 3897-907.
- 9) "Synthesis and Antifungal Activity of Cholesterol-Hydrazone Derivatives" Loncle, C.; Brunel, J. M.; Vidal, N.; Dherbomez, M.; Letourneux, Y. Eur. J. Med. Chem. 2004, 39, 1067-1071.
- 10) "BINOL : A Versatile Chiral Reagent" Brunel, J. M. Chem. Rev. 2005, 105, 857-897.
11) "New Efficient and Totally Stereoselective Copper Allylic Benzoyloxylation of Sterol Derivatives" Brunel, J. M. ; Billottet, L. ; Letourneux, Y. Tetrahedron Asymmetry 2005, 16, 3036-3041. - 12) "Pd/P(t-Bu)3: A mild catalyst for selective reduction of alkenes under transfer hydrogenation conditions" Brunel, J. M. Synlett 2007, 330-332.
- 13) "Squalamine: an appropriate strategy against the emergence of multidrug resistant Gram-negative bacteria?" Salmi, C.; Loncle, C.; Vidal, N.; Letourneux, Y.; Fantini, J.; Maresca, M. ; Taïeb, N. ; Pagès, J. M. ; Brunel, J. M. Plos One 2008, 3(7), e2765.
- 14) "In vitro antibacterial activity of aminosterols towards multidrug resistant bacteria from patients with cystic fibrosis" Alhanout, K.; Brunel, J. M.; Raoult, D.; Rolain, J. M. J. Antimicrob. Chemother. 2009, 64, 810-814.
- 15) "Modified Cap Group Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitor Derivatives Reveal Improved Selective Antileukemic Activity" Salmi-Smail, C.; Fabre, A.; Dequiedt, F.; Restouin, A.; Castellano, R.; Garbit, S.; Roche, P.; Morelli, X.; Brunel, J. M.; Collette, Y. J. Med. Chem. 2010, 53, 3038-3047.
- 16) "Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities" Djouhri, L .; Vidal, N.; Rolain, J. M.; Brunel, J. M. J. Med. Chem. 2011, 54, 7417-7421.
- 17) "Design of N-substituted aminobutyric hydroxamic acid histone deacetylase inhibitors reveal an essential role for cap atomic composition" Brunel, J. M.; Salmi-Smail, C.; Restouin, A.; Prébet, T.; Vey, N.; Collette, Y. Anticancer Agents Med. Chem. 2012, under Press.
Patents
- 1) "Preparation of diamino-o-tolylphosphines and their organometallic palladium complexes, methods of preparation and uses of complexes as catalysts for arylation of olefins." Brunel, J. M.; Buono, G.; Heumann, A. PCT Int. Appl. (2001), WO 2001007449.
- 2) "New process of synthesis of a squalamine and/or trodusquemine precursor." Brunel, J. M.; Vidal, N.; Pages, J. M.; Letourneux, Y. PCT Int. Appl. (2008), WO 2008110941.
- 3) "New process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. European patent N°08305954.3 (16/12/2008).
- 4) "New process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. US provisional patent N°61/122785 (16/12/2008).
- 5) "Process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. US provisional patent N°61/154105 (20/02/2009).
- 6) "Amino catalyzed production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. US provisional patent N°61/225726 (15/07/2009).
- 7) "New process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. PCT/EP2009/067309 (16/12/2009).
- 8) "Utilisation de composés aminostéroïdiens en application topique locale pour la décolonisation cutanéo-muqueuse de S. aureus". Brunel, J. M.; Rolain, J. M.; Raoult, D. European patent N°0958575 (02/12/2009).
- 9) "Phosphine-oxide catalyzed process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. US provisional patent N°61/304595 (15/02/2010).
- 10) "Use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment". Brunel, J. M.; Bolla, J. M. European patent N°11305193 (23/02/2011)
- 11) "Phosphine-oxide catalyzed process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. PCT/EP2011/052192 (15/02/2011).
- 12) "Compounds and methods for identifying and/or quantifying carbonylated biomolecules". Sellami, L.; Villard, C.; Brunel, J. M.; Lafitte, D. European patent N°11305567.7-2103 (11/05/2011).
- 13) "Phosphine- oxide catalyzed process of production of hydrogen from silylated derivatives as hydrogen carrier". Brunel, J. M. PCT Int. Appl. WO 2011098614 (2011).
- 14) "Aminosteroid compounds for topical application for decolonization of Staphylococcus aureus". Brunel, J. M.; Raoult, Didier; Rolain, Jean-Marc PCT Int. Appl. WO 2011067501 (2011).
- 15) "New apoptosis inducing compounds" Lopez, M.; Mezil, L.;Brunel, J. M.; Combes, S. ; Collette, Y. ; Birnbaum, D. European patent N°11306286.3 (04/10/2011). "Dérivés aminostéroïdiens anti-diabétiques" Brunel, J. M. ; Govers, R. European patent N°1159377 (17/10/2011).
- 16) "Utilisation de squalamine ou analogues comme agent désinfectant"Brunel, J. M.; Rolain, J. M.; Raoult, D. European patent N°1250312 (12/01/2012).
- 17) "Preparation of polyaminoisoprenyl derivatives for use in medical and nonmedical antibiotic or antiseptic treatment" Bolla, J. M.;Brunel, J. M.; Casanova, J. P. F.; Lorenzi, V.; Berti, L. PCT Int. Appl. WO 2012113891 (2012).
- 18) “Compounds and methods for identifying and/or quantifying carbonylated biomolecules” Sellami, L.; Villard, C.;Brunel, J. M.; Lafitte, D. PCT Int. Appl. WO 2012152943 (2012).
- 19) "Preparation of sulfonylthiomorpholine-3-carboxamides as apoptosis inducing compounds" Lopez, M.; Collette, Y.; Mezil, L.; Brunel, J. M.; Combes, S. PCT Int. Appl. WO 2013050476 (2013) (04/10/2012).
- 20) "Aminosteroid derivatives with substitutions at positions 3 and 6 for use in the treatment of insulin resistance and diabetes" Govers, R. M. T.; Brunel, J. M. Fr. Demande FR 2981351 (2013) (01/10/2012).
- 21) "Aminosteroid derivatives with substitutions at positions 3 and 6 for use in the treatment of insulin resistance and diabetes" Govers, R. M. T.; Brunel, J. M. PCT Int. Appl. WO 2013057422 (2013) (01/10/2012).
- 22) "Use of squalamine or analogue as a disinfecting agent" Brunel, J. M.; Raoult, D.; Rolain, J. M. PCT Int. Appl. WO 2013104849 (23/01/2013).
- 23) "Use of squalamine or its analogs as a disinfecting agent" Brunel, J. M.; Rolain, J. M.; Raoult, D. Fr. Demande FR 2985668 (2013).
Publications
- 1) "The Use of (4R,5R)-Dicarboalkoxy 2-Chloro 1,3,2-Dioxaphospholanes as New Chiral Derivatizing Reagents for the Determination of Enantiomeric Purity of Alcohols by 31P NMR." Brunel, J. M.; Maffei, M.; Pardigon, O.; Buono, G. Tetrahedron : Asymmetry 1992, 3, 1243-1246.
- 2) "Enantioselective Borane Reduction of Ketones Catalyzed by a Chiral Oxazaphospholidine Borane Complex" Brunel, J. M.; Faure, B.; Pardigon, O.; Buono, G. J. Chem. Soc., Chem. Commun. 1992, 287-288.
- 3) "Enantioselective Reduction of Ketones With Borane Catalyzed by (S)-(-)-Proline or (S)-(+)-Prolinol" Brunel, J. M.; Maffei, M.; Buono, G. Tetrahedron : Asymmetry 1993, 4, 2255-2260.
- 4) "Enantioselective Borane Reduction of Ketones Catalyzed by a Chiral Oxazaphospholidine Borane Complex" Buono, G.; Brunel, J. M.; Faure, B; Pardigon, O. Phosphorus, Sulfur and Silicon 1993, 75, 43-48.
- 5) "A New and Efficient Method for the Resolution of 1,1'-binaphthalene-2,2'-diol" Brunel, J. M.; Buono, G. J. Org. Chem. 1993, 58, 7313-7314.
- 6) "Structure of a (1R,4S)-O-Anisyl-2-oxa-3-aza-1-phosphabicyclo [3.3.0]octane-Borane Complex" Brunel, J. M.; Buono, G.; Baldy, A.; Declercq, J. P. Acta Crystallographica 1994, C50, 954-957.
- 7) "Synthesis of 2,3-Di-(acetoxymethyl)-Bicyclo[2.2.1]-Hepta-2,5-diene and Its Use in Palladium Catalysed Elimination" Muchow, G.; Brunel, J. M.; Maffei, M.; Buono, G. J. Org. Chem. 1995, 60, 852-855.
- 8) "A New 31P NMR Method for the Enantiomeric Excess Determination of Diols or Secondary Diamines with C2 Symmetry" Brunel, J. M.; Faure, B. Tetrahedron : Asymmetry 1995, 9, 2353-2356.
- 9) "Highly Enantioselective Oxidation of Sulfides Mediated by a Chiral Titanium Complex" Brunel, J. M.; Diter, P.; Duetsch, M.; Kagan, H. B. J. Org. Chem. 1995, 60, 8086-8088.
- 10) "Enantioselective Borane Catalyzed Reduction of Imines" Brunel, J. M.; Buono, G. Synlett 1996, 177-178.
- 11) "Catalytic Asymmetric Oxidation of Sulfides with High Enantioselectivities" Brunel, J. M.; Kagan, H. B. Synlett 1996, 404-406.
- 12) "Structure of a (2R,5S)-2,3-diphenyl-1,3-diaza phosphabicyclo-[3.3.0]-octane-borane complex" Brunel, J. M.; Buono, G.; Baldy, A.; Declercq, J. P. Acta Crystallographica 1996, C52, 1316-1317.
- 13) "Nuclear Overhauser Effects in Diastereoisomeric Vinyl Ethers for the Precise Structure Determination of Chiral Alcohols" Heumann, A.; Brunel, J. M.; Faure, R.; Kolshorn, H. J. Chem. Soc., Chem. Commun. 1996, 1159-1160.
- 14) "New Studies in Catalytic Asymmetric Oxidation of Sulfides" Brunel, J. M.; Kagan, H. B. Bull. Chem. Soc.Fr. 1996, 133, 1109-1115.
- 15) "Use of New Chiral Tricoordinated Phosphorus Borane Complexes in Enantioselective Borane Reduction of Ketones : Complexes Structure and Mechanistic Studies" Brunel, J. M.; Chiodi, O.; Faure, B.; Fotiadu, F.; Buono, G. J. Organomet. Chem. 1997, 529, 285-294.
- 16) "Enantioselective Palladium Catalyzed Allylic Substitution with New Chiral Pyridine Phosphine Ligands" Brunel, J. M.; Constantieux, T. ; Labande, A. ; Lubatti, F. ; Buono, G. Tetrahedron Lett. 1997, 38, 5971-5974.
- 17) "Enantioselective Palladium Catalyzed Allylic Amination Using New Chiral Pyridine-Phosphine Ligands" Constantieux, T. ; Brunel, J. M.; Labande, A. ; Buono, G. Synlett 1998, 49-50.
- 18) "Enzymatic Desymmetrization of Prochiral 2,3-bis(acetoxymethyl) bicyclo[2.2.1]hepta-2,5-diene and 2,3-bis(hydroxymethyl)bicyclo[2.2.1] hepta-2,5-diene" Ranchoux, M. ; Brunel, J. M.; Iacazio, G. ; Buono, G. Tetrahedron Asymmetry. 1998, 9, 581-587.
- 19) "Totally Stereoselective P-O to P-C Migration Rearrangement : Application to the Synthesis of New Chiral o-Hydroxyaryl Phosphine Oxides" Legrand, O. ; Brunel, J. M.; Constantieux, T. ; Buono, G. Chem. Eur. J. 1998, 4, 1061-1067.
- 20) "Pd(0) Catalyzed Asymmetric Amination of a Prochiral Bicyclic Allylic Diacetate" Muchow, G. ; Brunel, J. M.; Maffei, M. ; Pardigon, O. ; Buono, G. Tetrahedron 1998, 54, 10435-10448.
- 21) "New Chiral o-Hydroxyphenyl Diazaphospholidine Oxides. Catalytic Application in Asymmetric Addition of Diethylzinc to Aromatic Aldehydes" Brunel, J. M.; Constantieux, T. ; Legrand, O. ; Buono, G. Tetrahedron Lett. 1998, 39, 2961-2964.
- 22) "Nonlinear Effects as 'Indicators' in the Tuning of Asymmetric Catalysts" Brunel, J. M.; Luukas, T. O. ; Kagan, H. B. Tetrahedron Asymmetry 1998, 9, 1941-1946.
- 23) "Chiral o-Hydroxyarylphosphine Oxides : a New Family of Efficient Catalysts in Asymmetric Addition of Diethylzinc to Benzaldehyde" Legrand, O. ; Brunel, J. M. ; Buono, G. Tetrahedron Lett. 1998, 39, 9419-9422.
- 24) "Enantioselective Copper Catalyzed Diels-Alder Reaction Using Chiral Quinoline-Phosphine Ligand" Brunel, J. M. ; Del Campo, B. ; Buono, G. Tetrahedron Lett. 1998, 39, 9663-9666.
- 25) "Phosphane Boranes : Synthesis, Characterization and Synthetic Application" Brunel, J. M. , Faure, B. ; Maffei, M. Coord. Chem. Rev. 1998, 178-180, 665-698.
- 26) "Recent Advances in Asymmetric Copper Allylic Oxidation of Olefins" Brunel, J. M.; Legrand, O. ; Buono, G. C. R. Acad. Sc. Paris, t. 2, Série II 1999, 19-23.
- 27) "Synthesis of New Chiral s2l2-Phosphenium Cations" Brunel, J. M. ; Villard, R. ; Buono, G. Tetrahedron Lett. 1999, 40, 4669-4672.
- 28) "Enantioselective Rhodium Catalyzed Hydroboration of Olefins Using Chiral Bis(aminophosphine) Ligands" Brunel, J. M. ; Buono, G. Tetrahedron Lett. 1999, 40, 3561-3564.
- 29) "Totally Regio- and Stereoselective P-O to P-C Rearrangement in the Synthesis of Chiral P-(o-Hydroxyaryl)diazaphospholidine P-Oxides" Legrand, O. ; Brunel, J. M. ; Buono, G. Eur. J. Org. Chem. 1999, 1099-1105.
- 30) "New Ring Expansion Reaction of Chiral Diazaphospholidine Oxides via a Totally Stereospecific P-N to P-Csp2 Migration Rearrangement" Legrand, O. ; Brunel, J. M. ; Buono, G. Angew. Chem., Int. Ed. Engl. 1999, 38, 1479-1483.
- 31) "First Iminodiazaphospholidines with a Stereogenic Phosphorus Center. Efficient Ligands to Asymmetric Copper Catalyzed Cyclopropanation" Brunel, J. M. ; Legrand, O. ; Reymond, S. ; Buono, G. J. Am. Chem. Soc. 1999, 121, 5807-5808.
- 32) "Enantioselective Trimethylsilylcyanation of Aromatic Aldehydes Catalyzed by Titanium Alkoxide-Chiral o-Hydroxyarylphosphine Oxides Complexes" Brunel, J. M. ; Legrand, O. ; Buono, G. Tetrahedron : Asymmetry 1999, 10, 1979.
- 33) "Enantioselective Synthesis of (-)-Bifurcadiol : a Natural Antitumor Marine Product" Di Guardia, S. ; Valls, R. ; Mesguiche, V. ; Brunel, J. M. ; Culioli, G. Tetrahedron Lett. 1999, 40, 8359-8360.
- 34) "A Practical Method for the Large-Scale Synthesis of Diastereomerically Pure (2R,5S)- 3-Phenyl-2-(8-quinolinoxy)-1,3-diaza-2-phosphabicyclo-[3.3.0]-octane Ligand (QUIPHOS). Synthesis and X-ray Structure of Its Corresponding Chiral p-Allyl Palladium Complex" Brunel, J. M. ; Constantieux, T. ; Buono, G. J. Org. Chem. 1999, 64, 8940-8942.
- 35) "Scope and Limitations of the Aromatic Anionic [1,3] P-O to P-C Rearrangement in the Synthesis of Chiral o-Hydroxyaryldiazaphosphonamides" Legrand, O. ; Brunel, J. M. ; Buono, G. Tetrahedron 2000, 56, 285-293.
- 36) "Mechanistic Investigation into the Addition of Diethylzinc to Aromatic Aldehydes Catalyzed by Chiral o-Hydroxyaryldiazaphosphonamides" Legrand, O. ; Brunel, J. M. ; Buono, G. Tetrahedron Lett. 2000, 41, 2105-2109.
- 37) "Highly Efficient Phosphapalladacyclic Catalysts for the Hydroarylation of Norbornene" Brunel, J. M. ; Heumann, A. ; Buono, G. Angew. Chem., Int. Ed. Engl. 2000, 39, 1946-1949.
- 38) "New Chiral Organophosphorus Derivatizing Agent for the Determination of the Enantiomeric Composition of Chloro- and Bromohydrins by 31P NMR Spectroscopy" Reymond, S. ; Brunel, J. M. ; Buono, G. Tetrahedron Asymmetry 2000, 11, 1273-1278.
- 39) "Evidence of Formation of an exo-p-Allyl Complex Intermediate in the Pd0-Catalyzed Alkylation of a Bicyclic Allylic Diacetate with Stabilized Carbon Nucleophiles" Brunel, J. M. ; Maffei, M. ; Muchow, G. ; Buono, G. Eur. J. Org. Chem. 2000, 1799-1803.
- 40) "Enantioselective Conjugate Addition of Diethylzinc to Enones with Chiral Copper-QUIPHOS Catalyst. Influence of the Adddition of Water on the Enantioselectivity" Delapierre, G. ; Constantieux, T. ; Brunel, J. M. ; Buono, G. Eur. J. Org. Chem. 2000, 2507-2511.
- 41) "Chiral (o-Hydroxyaryl)oxazaphospholidine Oxides: A New Class of Bifunctional Catalysts in the Enantioselective Borane Reduction of Ketones" Brunel, J. M. ; Legrand, O. ; Buono, G. Eur. J. Org. Chem. 2000, 3313-3321.
- 42) "Enantioselective Formation of Quaternary Centers on b-Ketoesters with Chiral Palladium QUIPHOS Catalyst" Brunel, J. M. ; Tenaglia, A. ; Buono, G. Tetrahedron :Asymmetry 2000, 11, 3585-3590.
- 43) "Highly Efficient Phosphazene Base-Catalyzed Michael Addition of b-Ketoesters in Water" Bensa, D. ; Brunel, J. M. ; G. ; Buono, G. ; Rodriguez, J. Synlett 2001, 715-717.
- 44) "Experimental Evidence on the Existence of an exo-p-Allyl Complex Intermediate in the Pd0-Catalyzed Alkylation of a Bicyclic Allylic Diacetate with Stabilized Carbon Nucleophiles" Brunel, J. M. ; Maffei, M. ; Muchow, G. ; Buono, G. Eur. J. Org. Chem. 2001, 1009-1012.
- 45) "Une Nouvelle Classe de Ligands Chiraux : les Quinoléine-Phosphines. Synthèse et Application en Catalyse Asymétrique" Delapierre, G. ; Constantieux, T. ; Brunel, J. M. ; G. ; Buono, G. Quand Chemistry Devient Chimie 2001, 6-7.
- 46) "Design of a New Class of Chiral Quinoline-Phosphine Ligands. Synthesis and Application in Asymmetric Catalysis" Delapierre, G. ; Brunel, J. M. ; Constantieux, T. ; G. ; Buono, G. Tetrahedron :Asymmetry 2001, 1345-1352.
- 47) "New Chiral Organophosphorus Catalysts in Asymmetric Synthesis." Brunel, J. M. ; Buono, G. Topics Curr. Chem. 2002, 220, 79-105.
- 48) " Recent Advances in the Synthesis of Spermine and Spermidine Analogs of the Shark Aminosterol Squalamine " Brunel, J. M. ; Letourneux, Y. Eur : J. Org. Chem. 2003, 3897-907.
- 49) "Recent Advances in Asymmetric Reduction of Imines and Imine Derivatives" Brunel, J. M. Recent Res. Develop. Organic Chem. 2003, 155-190.
- 50) "Enantioselective Palladium Catalyzed Allylic Substitution with a New Phosphite Ligand Issued from (2S,5S)-Hexanediol " Brunel, J. M. ; Faure, B. J. Mol. Catal. A. 2004, 212, 61-64.
- 51) "Recent Advances in the Catalytic Asymmetric Cyanohydrin Syntheses " Brunel, J. M. ; Holmes, I.. Angew. Chem., Int. Ed. Engl. 2004, 43, 2752-2778.
- 52) "P(tert-Bu)3 : A Versatile and Efficient Ligand in Homogeneous Catalysis " Brunel, J. M. Mini-Rev. in Org. Chem. 2004, 1, 249-277.
- 53) "Synthesis and Antifungal Activity of Cholesterol-Hydrazone Derivatives" Loncle, C.; Brunel, J. M.; Vidal, N.; Dherbomez, M.; Letourneux, Y. Eur. J. Med. Chem. 2004, 39, 1067-1071.
- 54) "Efficient Method for the Synthesis of an Important Precursor of Constrained Peptides " Brunel, J. M. Protein and Peptide Letters 2005, 12, 281-282.
- 55) "Efficient Peptide Coupling Method of Conjugated Carboxylic Acids with Methyl Ester Amino Acids Hydrochloride. Application to the Synthesis of Fa-Met, an Important Enzymatic Substrate." Brunel, J. M.; Salmi, C.; Letourneux, Y. Tetrahedron Lett. 2005, 46, 217-220.
- 56) "BINOL : A Versatile Chiral Reagent" Brunel, J. M. Chem. Rev. 2005, 105, 857-897.
- 57) "Squalamine : A Polyvalent Drug of the Future?" Brunel, J. M. ; Salmi, C.; Loncle, C ; Vidal, N.; Letourneux, Y. Current Cancer Drug Targets 2005, 5, 267-272.
- 58) "Maackiain 3-O-(6'-O-malonyl-b-D-glucopyranoside) from Oudneya Africana, a powerful inhibitor of porcine kidney acylase I" Stocker, P.; Yousfi, M.; Salmi, C.; Perrier, J.; Brunel, J. M.; Moulin, A. Biochimie 2005, 87, 507-512.
- 59) "Isolation and Characterization of New Tetrahydropyranyl Substituted Sesquiterpene and Myrmekiodermin Glycolipid Ether Isolated from the Marine Sponge Myrmekioderma " Letourneux, Y.; Brunel, J. M.; Fernandez, R.; Dherbomez, M.; Debitus, C. Heterocyclic Commun. 2005, 11, 291-298.
- 60) "Synthesis and Antifungal Activity of Oxygenated Cholesterol Derivatives" Brunel, J. M.; Loncle, C.; Vidal, N.; Dherbomez, M.; Letourneux, Y. Steroids 2005, 70, 907-912.
- 61) "Scope and Limitations of an Efficient Peptide Coupling Method for the Synthesis of N-Furylamino and N-Feruloylamino Acid Derivatives. Application to the Synthesis of Natural Antioxidant trans-Clovamide" Salmi, C.; Brunel, J. M.; Vidal, N.; Letourneux, Y. Lett. Org. Chem. 2005, 2, 398-403.
- 62) "New Efficient and Totally Stereoselective Copper Allylic Benzoyloxylation of Sterol Derivatives" Brunel, J. M. ; Billottet, L. ; Letourneux, Y. Tetrahedron Asymmetry 2005, 16, 3036-3041.
- 63) "Synthesis of 7-Dehydrocholesterol Through a Palladium Catalyzed Selective Homoannular Conjugated Diene Formation" Dugas, D.; Brunel, J. M. J. Mol. Catal. A 2006, 253, 119-122.
- 64) "Efficient Diastereoselective Titanium(IV) Reductive Amination of Ketones" Salmi, C.; Letourneux, Y. ; Brunel, J. M. Lett. Org. Chem. 2006, 3, 384-389.
- 65) "Efficient Synthesis of Various Secondary Amines Through a Titanium(IV)isopropoxide-Mediated Reductive Amination of Ketones" Salmi, C.; Letourneux, Y. ; Brunel, J. M. Lett. Org. Chem. 2006, 3, 396-401.
- 66) "Synthesis, Physical Characterization, Antibacterial and Antifungal activities of a novel bis(3-((E)-1-(2-hydroxyphenyl)ethylideneamino)phenyl) methanone" Jalbout, A. F. ; Jarrahpour, A. A.; Brunel, J. M.; Salmi, C.; Rezaei, S.; Trzaskowski, B. Molbank 2006, M484.
- 67) "Synthesis, Physical Characterization, Antibacterial and Antifungal Activities of 2-((E)-1-(2-((E)-1-(2-Hydroxyphenyl)ethylideneamino) phenylamino) ethyl) phenol" Jarrahpour, A. A.; Jalbout, A. F. ; Brunel, J. M.; Loncle, C.; Rezaei, S.; Trzaskowski, B. Molbank 2006, M489.
- 68) "Pd/P(t-Bu)3: A mild catalyst for selective reduction of alkenes under transfer hydrogenation conditions" Brunel, J. M. Synlett 2007, 330-332.
- 69) "Scope limitations and mechanistic aspects in the selective homogeneous palladium-catalyzed reduction of alkenes under transfer hydrogen conditions" Brunel, J. M. Tetrahedron 2007, 63, 330-332.
- 70) "Therapeutic potential of cationic steroid antibacterials" Salmi, C.; Brunel, J. M. Exp. Opin. Investig. Drugs 2007 16, 1143-1157.
- 71) "Synthesis, antibacterial, antifungal and antiviral activity. evaluation of some new bis-Schiff bases of isatin and their derivatives" Jarrahpour, A., Khalili, D., De Clercq, E., Salmi, C., Brunel, J. M. Molecules 2007, 12, 1720-1730.
- 72) "Update 1: BINOL : A Versatile Chiral Reagent" Brunel, J. M. Chem. Rev. 2007, 107, PR1-PR45.
- 73) "Synthesis of new 7-aminosterol squalamine analogues with high antimicrobial activities through a stereoselective titanium reductive amination reaction" Loncle, C., Salmi, C., Letourneux, Y., Brunel, J. M. Tetrahedron 2007, 63, 12968–12974.
- 74) "Inhibition of porcine liver carboxylesterase by a new flavone glucoside isolated from Deverra scoparia" Djeridane, A.; Brunel, J. M.; Vidal, N.; Yousfi, M.; Ajandouz, E. H.; Stocker, P. Chem. Biol. Interact. 2008, 172, 22-26.
- 75) "New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities » Salmi, C. ; Loncle, C. ; Vidal, N. ; Letourneux, Y. ; Brunel, J. M. Eur. J. Med. Chem., 2008, 43, 540-547.
- 76) "Efficient preparation of secondary aminoalcohols through a Ti(IV) reductive amination procedure. Application to the synthesis and antibacterial evaluation of new 3β-N-[hydroxyalkyl]aminosteroid derivatives" Salmi, C.; Loncle, C.; Letourneux, Y.; Brunel, J. M. Tetrahedron 2008, 64, 4453-4459.
- 77) "New 3-aminosteroid derivatives as a new family of topical antibacterial agents active against methicillin-resistant staphylococcus aureus (MRSA)" Salmi, C.; Loncle, C.; Vidal, N.; Laget, M.; Letourneux, Y.; Brunel, J. M. Lett. Drug Design & Discovery 2008, 5, 169-172.
- 78) "Squalamine: an appropriate strategy against the emergence of multidrug resistant Gram-negative bacteria?" Salmi, C.; Loncle, C.; Vidal, N.; Letourneux, Y.; Fantini, J.; Maresca, M. ; Taïeb, N. ; Pagès, J. M. ; Brunel, J. M. Plos One 2008, 3(7), e2765.
- 79) "Antimicrobial activities of 7-aminosterol squalamine analogues" Loncle, C.; Salmi, C.; Vidal, N.; Letourneux, Y.; Brunel, J. M. Lett. Drug Design & Discovery 2008, 5, 388-393.
- 80) "Antimicrobial Activities of 3-Amino- and Polyaminosterol Analogues of Squalamine and Trodusquemine" Salmi, C.; Loncle, C.; Vidal, N.; Laget, M.; Letourneux, Y. ; Brunel, J. M. J. Enzym Inhib. Med. Chem. 2008, 23, 860-865.
- 81) "In vitro antibacterial activity of aminosterols towards multidrug resistant bacteria from patients with cystic fibrosis" Alhanout, K.; Brunel, J. M.; Raoult, D.; Rolain, J. M. J. Antimicrob. Chemother. 2009, 64, 810-814.
- 82) "3-Aminosterol Compounds as a New Class of Anti-Malarial Agents against Chloroquine-Susceptible and -Resistant Plasmodium falciparum" Salmi, C.; Loncle, C.; Vidal, N.; Rogier, C.; Letourneux, Y.; Pradines, B.; Brunel, J. M. Lett. Drug Design & Discovery, 2009, 6, 163-166.
- 83) "Biophysical studies of the interaction of squalamine and other cationic amphiphilic molecules with bacterial and eukaryotic membranes: importance of the distribution coefficient in membrane selectivity" Di Pasquale, E.; Salmi-Smail, C.; Brunel, J. M.; Sanchez, P.; Fantini, J.; Maresca, M. Chem. Phys. Lipids 2010, 163, 131-140.
- 84) "A comparison of three rapid and accurate bioluminescent antibiotic susceptibility tests" Lafond, M.; Vidal, N.; Letourneux, Y.; Brunel, J. M. J. Pharmacol. Toxicol. Methods 2010, 61, 16–19.
- 85) "Modified Cap Group Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitor Derivatives Reveal Improved Selective Antileukemic Activity" Salmi-Smail, C.; Fabre, A.; Dequiedt, F.; Restouin, A.; Castellano, R.; Garbit, S.; Roche, P.; Morelli, X.; Brunel, J. M.; Collette, Y. J. Med. Chem. 2010, 53, 3038-3047.
- 86) "Squalamine, an original chemosensitizer to combat antibiotic-resistant Gram-negative bacteria" Lavigne, J. P.; Brunel, J. M.; Chevalier, J.; Pages, J. M. J. Antimicrob. Chemother. 2010, 65, 799-801.
- 87) "New efficient hydrogen process production from organosilane hydrogen carriers derivatives" Brunel, J. M. Int. J. Hydrogen Energy 2010, 35, 3401-3405.
- 88) "In vitro antifungal activity of aminosterols against moulds isolated from cystic fibrosis patients" Alhanout, K.; Brunel, J. M.; Ranque, S.; Rolain, J. M. J. Antimicrob. Chemother. 2010, 65, 1307-1309.
- 89) "Isolation and characterization of a new steroid derivative as a powerful antioxidant from Cleome arabica in screening the in vitro antioxidant capacity of 18 Algerian medicinal plants" Djeridane, A.; Yousfi, M.; Brunel, J. M.; Stocker, P. Food Chem.Toxicol. 2010, 48, 2599-2606.
- 90) "New insights into the antibacterial mechanism of action of squalamine" Alhanout, K.; Malesinki, S.; Vidal, N.; Peyrot, V.; Rolain, J. M.; Brunel, J. M. J. Antimicrob. Chemother. 2010, 65, 1688-1693.
- 91) "Squalamine as an example of a new potent antimicrobial agents class: a critical review" Alhanout, K.; Rolain, J. M.; Brunel, J. M. Curr. Med. Chem. 2010, 17, 3909-3917
- 92) "In vitro activity of aminosterols against yeasts involved in blood stream infections" Alhanout K, Djouhri L, Vidal N, Brunel J. M., Piarroux R, Ranque S. Med Mycol. 2011, 49, 121-125. 93) "New insights into the antibacterial mechanism of action of squalamine" Alhanout, K.; Malesinki, S.; Vidal, N.; Peyrot, V.; Rolain, J. M.; Brunel, J. M. J. Antimicrob. Chemother. 2011, 66, 1306-1310.
- 94) "Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities" Djouhri, L .; Vidal, N.; Rolain, J. M.; Brunel, J. M. J. Med. Chem. 2011, 54, 7417-7421.
- 95) "Synthesis of mono-, bis-spiro- and dispiro-b-lactams and evaluation of their antimalarial activities" Jarrahpour, A.; Ebrahimi, E.; De Clercq, E.; Sinou, V.; Latour, C.; Djouhri, L.; Brunel, J. M. Tetrahedron 2011, 67, 8699-8704.
- 96) "Suitability of a new antimicrobial aminosterol formulation for aerosol delivery in cystic fibrosis" Alhanout, K; Brunel, J. M.; Dubus, J. C.; Rolain, J. M.; Andrieu, V. J. Antimicrob. Chemother. 2011, 66, 2797-2800
- 97) "Synergistic activity of sulbactam combined with colistin against colistin-resistant Acinetobacter baumanni" Kempf, M.; Djouhri-Bouktab, L.; Brunel, J. M.; Raoult, D.; Rolain, J. M. Int J Antimicrob Agents. 2012, 39, 180-181.
- 98) "Synthesis of novel b-lactams bearing an anthraquinone moiety and evaluation of their antimalarial activities" Jarrahpour, A.; Ebrahimi, E.; Khalifeh, R.; Sharghi, H.; Sahraei, M.; Sinou, V.; Latour, C.; Brunel, J. M.Tetrahedron 2012, 68, 4740-4744
- 99) “Rapid Detection of Carbapenem Resistance in Acinetobacter baumannii Using Matrix-Assisted Laser Desorption Ionization-Time of Flight Mass Spectrometry” Kempf, M.; Bakour, S.; Flaudrops, C.; Berrazeg, M.; Brunel, J. M.; Drissi, M.; Mesli, E.; Touati, A.; Rolain, J. M. Plos One 2012, 7, e31676.
- 100) “Aminoacylase 1-catalysed deacetylation of bioactives epoxides mycotoxin-derived mercapturates ; 3,4-epoxyprecocenes as models of cytotoxic epoxides” Stocker, P.; Brunel, J. M.; de Rezende, L.; do Amaral, T.; Morelli, X.; Roche, P.; Vidal, N.; Giardina, T.; Perrier, J: Biochimie 2012, 94, 16658-1675.
- 101) "Design of N-substituted aminocaproic hydroxamic acid histone deacetylase inhibitors reveal an essential role for cap atomic composition" Brunel, J. M.; Salmi-Smail, C.; Restouin, A.; Prébet, T.; Vey, N.; Collette, Y. Anticancer Agents Med. Chem. 2012, 12, 801-806.
- 102) "Antibacterial efficacy of inhaled squalamine in a rat model of chronic Pseudomonas aeruginosa pneumonia” Hraiech, S.; Brégeon, F.; Brunel, J. M.; Rolain, J. M.; Lepidi, H.; Andrieu, V.; Raoult, D.; Papazian, L.; Roch, A. J. Antimicrob. Chemother. 2012, 67, 2452-2458.
- 103) "Soluble squalamine tablets for the rapid disinfection of home nebulizers of cystic fibrosis patients" Djouhri-Bouktab, L.; Alhanout, K.; Andrieu, V.; Stremler, N.; Dubus, J. C.; Raoult, D.; Rolain, J. M.; Brunel, J. M. J. Cyst. Fibros. 2012, 11, 555-559
- 104) "Tumor Selective Cytotoxic Action of a Thiomorpholin Hydroxamate Inhibitor (TMI-1) in Breast Cancer" Mezil, L.; Berruyer-Pouyet, C.; Cabaud, O.; Josselin, E.; Combes, S.; Brunel, J. M.; Viens, P.; Collette, Y.; Birnbaum, D.; Lopez, M. Plos One 2012, 7, e43409.
- 105) "Colistin: an update of the antibiotic of the 21st century" Biswas, S.; Brunel, J. M.; Dubus J. C.; Reynaud-Gaubert, M.; Rolain, J. M. Expert Rev. Anti Infect. Ther. 2012, 10, 917-934.
- 106) "Polyamino geranic derivatives as new chemosensitizers to combat antibiotic resistant Gram-negative bacteria" Brunel, J. M.; Lieutaud, A.; Lome, V.; Pagès, J. M.; Bolla, J. M. Bioorg. Med. Chem. 2013, 21, 1174-1179.
- 107) "Palmitoylation of TNF alpha is involved in the regulation of TNF receptor 1 signalling" Poggi, M.; Kara, I.; Brunel, J. M.; Landrier, J. F.; Govers, R.; Bonardo, B.; Fluhrer, R.; Haass, C.; Alessi, M. C.; Peiretti, F. Biochim. Biophys. Acta 2013, 1833, 602-612.
- 108)"In vitro activity of aminosterols against dermatophytes" Coulibaly, O.; Alhanout, K.; L'ollivier, C.; Brunel, J. M.; Thera, M. A.; Djimdé, A. A.; Doumbo, O. K.; Piarroux, R.; Ranque, S. Med Mycol. 2013, 51, 309-312.
- 109) "Hydrophobicity of imidazole derivatives correlates with improved activity against human methanogenic archaea" Khelaifia, S.; Brunel, J. M.; Raoult, D.; Drancourt, M. Int. J. Antimicrob. Agents 2013, 41, 544-547.
- 110) "2P2Ichem: focused chemical libraries dedicated to orthosteric modulation of protein-protein interactions" Hamon, V.; Brunel, J. M.; Combes, S.; Basse, M. J.; Roche, P.; Morelli, X. Med. Chem. Commun. 2013, 4, 797-809.
- 111) "In-vitro archaeacidal activity of biocides against human-associated archaea" Khelaifia, S.; Brunel, J. M.; Drancourt, M. PLoS One 2013, 8, e62738.
- 112) "In vitro antimicrobial activity of squalamine derivatives against mycobacteria" Ghodbane, R.; Ameen, S. M.; Drancourt, M.; Brunel, J. M. Tuberculosis 2013, 93, 565-566.
- 113) "The LIM domain only 4 protein is a metabolic responsive inhibitor of protein tyrosine phosphatase 1B that controls hypothalamic leptin signaling" Pandey, N. R.; Zhou, X.; Qin, Z.; Zaman, T.; Gomez-Smith, M.; Keyhanian, K.; Anisman, H.; Brunel, J. M.; Stewart, A. F. R.; Chen, H. H. J. Neuroscience 2013, 33, 12647-12655
- 114) "Pd0-Catalyzed Hydrogenolysis of a Bicyclic Allylic Diacetate" Muchow, G.; Brunel, J. M. Eur. J. Org. Chem. 2013, 6449-6454.
- 115) "Impaired virulence and fitness of a colistin-resistant clinical isolate of Acinetobacter baumannii in a rat model of Pneumonia" Hraiech, S.; Roch, A.; Lepidi, H.; Atieh, T.; Audoly, G.; Rolain, J. M.; Raoult, D.; Brunel, J. M.; Papazian, L.; Bregeon, F. Antimicrob. Agents Chemother 2013, 57, 5120-5121.
- 116) "Inhibitors of antibiotic efflux by AcrAB-TolC in Enterobacter aerogenes" Lieutaud, A.; Guinoiseau, E.; Lorenzi, V.; Giuliani, M. C.; Lome, V.; Brunel, J. M.; Luciani, A.; Casanova, J.; Pages, J-M.; Berti, L.; Bolla, J. M. Anti-Infective Agents 2013, 11, 168-178.
- 117) "New ianthelliformisamine derivatives as antibiotic enhancers against resistant gram-negative bacteria" Pieri, C.; Borselli, D.; Di Giorgio, C.; De Meo, M.; Bolla, J. M.; Vidal, N.; Combes, S.; Brunel, J. M. J. Med. Chem. 2014, 57, 4263-4272.
- 118) "2P2IHUNTER: a tool for filtering orthosteric protein - protein interaction modulators via a dedicated support vector machine" Hamon, V.; Bourges, R.; Ducrot, P.; Theret, I.; Xuereb, L.; Basse, M. J.; Brunel, J. M.; Combes, S.; Moreli, X.; Roche, P. J. Royal Soc., Interface 2014, 11, 20130860/1-20130860/11.
- 119) "Mini-Review: Polyamines Metabolism, Toxicity and Potent Therapeutical Use" Djouhri-Bouktab, L.; Rolain, J. M.; Brunel, J. M. Anti-Infective Agents 2014, 12 , 95-103
- 120) "Non-Genotoxic Assessment of a Natural Antimicrobial Agent: Squalamine" Alhanout, K.; Di Giorgio, C.; De Meo, M.; Brunel, J. M. Anti-Infective Agents 2014, 12, 75-79