Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis
Flipo, Marion
Willand, Nicolas
Lecat-Guillet, Nathalie
Hounsou, Candide
Desroses, Matthieu
Leroux, Florence
Lens, Zoe
Villeret, Vincent
Wohlkonig, Alexandre
Wintjens, Rene
Christophe, Thierry
Jeon, Hee Kyoung
Locht, Camille
Brodin, Priscille
Baulard, Alain R.
Deprez, Benoit
Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
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Benoit Deprez
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Synthesis of a 200-member library of squaric acid N-hydroxylamide amides
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Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents
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Facts, figures and trends in lead generation
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From hit to lead. Analyzing structure-profile relationships
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Orthogonal combinatorial chemical libraries
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Pimelautide or trimexautide as built-in adjuvants associated with an HIV- 1-derived peptide: Synthesis and in vivo induction of antibody and virus- specific cytotoxic T-lymphocyte-mediated response
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Marion Flipo
Flipo Marion
ORCID: 0000-0003-2863-5721
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Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery
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Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-beta hydrolysis
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Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches
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Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands
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On the Mechanism of Degradation of Oxytocin and its Analogues in Aqueous Solution
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Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis
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Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors
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Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors
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Tuberculosis: The drug development pipeline at a glance
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Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors
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Hydroxamates: Relationships between Structure and Plasma Stability
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A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening
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Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents
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Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis
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A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity
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Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening
10.1016/j.ejmech.2020.112440
florence leroux
leroux florence
ORCID: 0000-0003-0554-873X
Synthetic EthR inhibitors boost antituberculous activity of ethionamide
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Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors
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Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds
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Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds
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Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors
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Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis
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Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation
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Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors
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Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis
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Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737
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Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group
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Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches
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Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance
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Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme
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Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism
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Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice
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ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity
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Drug Target Engagement Using Coupled Cellular Thermal Shift Assay-Acoustic Reverse-Phase Protein Array
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Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox
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A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2
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HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF CYCLIC 3',5'-AMP WITH FLUORESCENCE DETECTION - VASOACTIVE INTESTINAL PEPTIDE-INDUCED MODIFICATION OF ITS CONCENTRATION IN NEUROBLASTOMA-CELLS
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A NEW VASOACTIVE-INTESTINAL-PEPTIDE ANTAGONIST DISCRIMINATES VIP RECEPTORS ON GUINEA-PIG TRACHEA AND HUMAN NEUROBLASTOMA-CELLS
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Tracheal Relaxant Effect of Triazine Derivatives: Correlation with Phosphodiesterase 4 Inhibitory Activity
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Use of a low-density microarray for studying gene expression patterns induced by hepatotoxicants on primary cultures of rat hepatocytes
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High-Throughput Image-Based Aggresome Quantification
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