Search Results - "Déprez, Benoit"

Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space by Prevet, Hugues, Flipo, Marion, Roussel, Pascal, Deprez, Benoit, Willand, Nicolas

“…[Display omitted] •Rapid chemical pathway for the synthesis of new 3D privileged fragments.•Microwave-assisted synthesis of a large set of…”
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Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis by Prieri, Marion, Frita, Rosangela, Probst, Nicolas, Sournia-Saquet, Alix, Bourotte, Marilyne, Déprez, Benoit, Baulard, Alain R., Willand, Nicolas

“…Ethionamide is a key antibiotic prodrug of the second-line chemotherapy regimen to treat tuberculosis. It targets the biosynthesis of mycolic acids thanks to a…”
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Access to newly functionalized imidazole derivatives: efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P) by Lasalle, Manuel, Picon, Sylvain, Boulahjar, Rajaa, Hoguet, Vanessa, Van Obbergen, Jolien, Roussel, Pascal, Deprez, Benoit, Charton, Julie

“…[Display omitted] We describe here an efficient method to synthesize 5-amino-2-thioimidazole compounds by T3P-mediated cyclization of N-acetamidoisothiourea…”
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Novel Selective Inhibitors of the Zinc Plasmodial Aminopeptidase PfA-M1 as Potential Antimalarial Agents by Flipo, Marion, Beghyn, Terence, Leroux, Virginie, Florent, Isabelle, Deprez, Benoit P, Deprez-Poulain, Rebecca F

“…Proteases that are expressed during the erythocytic stage of Plasmodium falciparum are newly explored drug targets for the treatment of malaria. We report here…”
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Novel non-carboxylic acid retinoids: 1,2,4-Oxadiazol-5-one derivatives by Charton, Julie, Deprez-Poulain, Rebecca, Hennuyer, Nathalie, Tailleux, Anne, Staels, Bart, Deprez, Benoit

“…We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays an EC50 of 26 nM on…”
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A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening by Flipo, Marion, Beghyn, Terence, Charton, Julie, Leroux, Virginie A., Deprez, Benoit P., Deprez-Poulain, Rebecca F.

“…We report here the design and parallel synthesis of 217 compounds based on a malonic–hydroxamic acid template. These compounds are obtained via a two-step…”
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Microwave‐Assisted Suzuki‐Miyaura Cross Coupling using Nickel as Catalyst to Rapidly Access to 3‐Arylazetidine by Dequirez, Geoffroy, Bourotte, Marilyne, Porras de Francisco, Esther, Remuiñan Blanco, Modesto J., Déprez, Benoit, Willand, Nicolas

“…The efficient synthesis of 3‐arylazetidine derivatives is reported using a Nickel‐catalyzed Suzuki‐Miyaura coupling between arylboronic acids and a…”
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UFU (‘Ullmann–Finkelstein–Ullmann’): a new multicomponent reaction by Toto, Patrick, Gesquière, Jean-Claude, Cousaert, Nicolas, Deprez, Benoit, Willand, Nicolas

“…The development of a Ullmann–Finkelstein–Ullmann multicomponent reaction and its application to the synthesis of nonsymmetrical para-disubstituted benzene…”
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Rescue of nonsense mutations by amlexanox in human cells by Gonzalez-Hilarion, Sara, Beghyn, Terence, Jia, Jieshuang, Debreuck, Nadège, Berte, Gonzague, Mamchaoui, Kamel, Mouly, Vincent, Gruenert, Dieter C, Déprez, Benoit, Lejeune, Fabrice

“…Nonsense mutations are at the origin of many cancers and inherited genetic diseases. The consequence of nonsense mutations is often the absence of mutant gene…”
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Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps by Plé, Coline, Tam, Heng-Keat, Vieira Da Cruz, Anais, Compagne, Nina, Jiménez-Castellanos, Juan-Carlos, Müller, Reinke T., Pradel, Elizabeth, Foong, Wuen Ee, Malloci, Giuliano, Ballée, Alexia, Kirchner, Moritz A., Moshfegh, Parisa, Herledan, Adrien, Herrmann, Andrea, Deprez, Benoit, Willand, Nicolas, Vargiu, Attilio Vittorio, Pos, Klaas M., Flipo, Marion, Hartkoorn, Ruben C.

“…Efflux transporters of the RND family confer resistance to multiple antibiotics in Gram-negative bacteria. Here, we identify and chemically optimize…”
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Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles by Costa-Gouveia, Joana, Pancani, Elisabetta, Jouny, Samuel, Machelart, Arnaud, Delorme, Vincent, Salzano, Giuseppina, Iantomasi, Raffaella, Piveteau, Catherine, Queval, Christophe J., Song, Ok-Ryul, Flipo, Marion, Deprez, Benoit, Saint-André, Jean-Paul, Hureaux, José, Majlessi, Laleh, Willand, Nicolas, Baulard, Alain, Brodin, Priscille, Gref, Ruxandra

“…Tuberculosis (TB) is a leading infectious cause of death worldwide. The use of ethionamide (ETH), a main second line anti-TB drug, is hampered by its severe…”
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Optimization of 1,2,4-Triazole-3-thiones toward Broad-Spectrum Metallo-β-lactamase Inhibitors Showing Potent Synergistic Activity on VIM- and NDM-1-Producing Clinical Isolates by Legru, Alice, Verdirosa, Federica, Vo-Hoang, Yen, Tassone, Giusy, Vascon, Filippo, Thomas, Caitlyn A., Sannio, Filomena, Corsica, Giuseppina, Benvenuti, Manuela, Feller, Georges, Coulon, Rémi, Marcoccia, Francesca, Devente, Savannah Rowane, Bouajila, Ezeddine, Piveteau, Catherine, Leroux, Florence, Deprez-Poulain, Rebecca, Deprez, Benoît, Licznar-Fajardo, Patricia, Crowder, Michael W., Cendron, Laura, Pozzi, Cecilia, Mangani, Stefano, Docquier, Jean-Denis, Hernandez, Jean-François, Gavara, Laurent

“…Metallo-β-lactamases (MBLs) contribute to the resistance of Gram-negative bacteria to carbapenems, last-resort antibiotics at hospital, and MBL inhibitors are…”
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The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity by Broeders, Evie P.M., Nascimento, Emmani B.M., Havekes, Bas, Brans, Boudewijn, Roumans, Kay H.M., Tailleux, Anne, Schaart, Gert, Kouach, Mostafa, Charton, Julie, Deprez, Benoit, Bouvy, Nicole D., Mottaghy, Felix, Staels, Bart, van Marken Lichtenbelt, Wouter D., Schrauwen, Patrick

“…The interest in brown adipose tissue (BAT) as a target to combat metabolic disease has recently been renewed with the discovery of functional BAT in humans. In…”
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Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration by Antraygues, Kevin, Maingot, Mathieu, Schellhorn, Birgit, Trebosc, Vincent, Gitzinger, Marc, Deprez, Benoit, Defert, Olivier, Dale, Glenn E., Bourotte, Marilyne, Lociuro, Sergio, Willand, Nicolas

“…Acinetobacter baumannii is a gram-negative bacterium causing severe hospital-acquired infections such as bloodstream infections or pneumonia. Moreover,…”
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Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles by Wen, Xiaoan, Bakali, Jamal El, Deprez-Poulain, Rebecca, Deprez, Benoit

“…Propylphosphonic anhydride (®T3P) promotes cyclization of o-aminobenzenethiol, o-aminophenol, and o-phenylenediamine with carboxylic acids under microwave…”
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Efficient, protection-free Suzuki–Miyaura synthesis of ortho-biphenyltetrazoles by Cousaert, Nicolas, Toto, Patrick, Willand, Nicolas, Deprez, Benoît

“…We describe an efficient protocol for the Suzuki–Miyaura synthesis of ortho-biphenyltetrazoles from non-protected 2-bromophenyltetrazole and arylboronic acids…”
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Tuberculosis: The drug development pipeline at a glance by Villemagne, Baptiste, Crauste, Céline, Flipo, Marion, Baulard, Alain R., Déprez, Benoit, Willand, Nicolas

“…Tuberculosis is a major disease causing every year 1.8 million deaths worldwide and represents the leading cause of mortality resulting from a bacterial…”
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Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice by Deprez-Poulain, Rebecca, Hennuyer, Nathalie, Bosc, Damien, Liang, Wenguang G., Enée, Emmanuelle, Marechal, Xavier, Charton, Julie, Totobenazara, Jane, Berte, Gonzague, Jahklal, Jouda, Verdelet, Tristan, Dumont, Julie, Dassonneville, Sandrine, Woitrain, Eloise, Gauriot, Marion, Paquet, Charlotte, Duplan, Isabelle, Hermant, Paul, Cantrelle, François- Xavier, Sevin, Emmanuel, Culot, Maxime, Landry, Valerie, Herledan, Adrien, Piveteau, Catherine, Lippens, Guy, Leroux, Florence, Tang, Wei-Jen, van Endert, Peter, Staels, Bart, Deprez, Benoit

“…Insulin-degrading enzyme (IDE) is a protease that cleaves insulin and other bioactive peptides such as amyloid-β. Knockout and genetic studies have linked IDE…”
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NMR Spectroscopy of the Main Protease of SARS‐CoV‐2 and Fragment‐Based Screening Identify Three Protein Hotspots and an Antiviral Fragment by Cantrelle, François‐Xavier, Boll, Emmanuelle, Brier, Lucile, Moschidi, Danai, Belouzard, Sandrine, Landry, Valérie, Leroux, Florence, Dewitte, Frédérique, Landrieu, Isabelle, Dubuisson, Jean, Deprez, Benoit, Charton, Julie, Hanoulle, Xavier

“…The main protease (3CLp) of the SARS‐CoV‐2, the causative agent for the COVID‐19 pandemic, is one of the main targets for drug development. To be active, 3CLp…”
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Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 by Blondiaux, Nicolas, Moune, Martin, Desroses, Matthieu, Frita, Rosangela, Flipo, Marion, Mathys, Vanessa, Soetaert, Karine, Kiass, Mehdi, Delorme, Vincent, Djaout, Kamel, Trebosc, Vincent, Kemmer, Christian, Wintjens, René, Wohlkönig, Alexandre, Antoine, Rudy, Huot, Ludovic, Hot, David, Coscolla, Mireia, Feldmann, Julia, Gagneux, Sebastien, Locht, Camille, Brodin, Priscille, Gitzinger, Marc, Déprez, Benoit, Willand, Nicolas, Baulard, Alain R.

“…Antibiotic resistance is one of the biggest threats to human health globally. Alarmingly, multidrug-resistant and extensively drug-resistant Mycobacterium…”
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