Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes R. Rajeshwari, V. Duvauchelle, C. Lindgren, K. Stangner, S. Knutsson, et al. Rsc Medicinal Chemistry, 2026 Four indole-based compounds demonstrated strong insecticidal effects against mosquitoes by acetylcholinesterase (AChE) inhibition. A selective profile over human AChE suggests a promising alternative in the development of future insecticides.
Characterization of Alginates of Sargassum from the Archipelago of Guadeloupe Naika Marcin, Valendy Thesnor, Valentin Duvauchelle, Alejandro Ponce-Mora, Lucia Gimeno-Mallench, et al. Separations, 2024 Sargassum is a genus of brown algae that causes a major impact to marine ecosystems. Although accumulation of this invasive seaweed is considered an environmental problem, Sargassum can also be resource of valuable molecules such as alginates. Alginates are polysaccharides extracted from the cell walls of brown seaweeds with multiple applications in food, cosmetics, pharmaceuticals, and biotechnology. In this study, we explored four different extraction protocols to isolate alginates from Sargassum from the archipelago of Guadeloupe. H-NMR, FTIR, and SEM were carried out to characterize isolated samples and describe their chemical and morphological properties. Antioxidant capacity of the isolated alginates was tested in the sample. FRAP assay showed free radical scavenging activity, and cell viability assay showed that alginates keep protective capacity against oxidative stress in cell cultures. In sum, the isolation methods used in this study are effective extractive methods to obtain alginates from Sargassum, which highlight this seaweed as a potential source of bioactive compounds that may be exploited for industrial and biomedical purposes.
Second-Generation CD73 Inhibitors Based on a 4,6-Biaryl-2-thiopyridine Scaffold Rayane Ghoteimi, Abdennour Braka, Céline Rodriguez, Emeline Cros‐Perrial, Valentin Duvauchelle, et al. Chemmedchem, 2023 Various series of 4,6‐biaryl‐2‐thiopyridine derivatives were synthesized and evaluated as potential ecto‐5′‐nucleotidase (CD73) inhibitors. Two synthetic routes were explored and the coupling of 4,6‐disubstituted 3‐cyano‐2‐chloro‐pyridines with selected thiols allowed us to explore the structural diversity. Somehow divergent results were obtained in biological assays on CD73 inhibition using either the purified recombinant protein or cell‐based assays, highlighting the difficulty to target protein‐protein interface on proteins existing as soluble and membrane‐bound forms. Among the 18 new derivatives obtained, three derivatives incorporating morpholino substituents on the 4,6‐biaryl‐2‐thiopyridine core were shown to be able to reverse the adenosine‐mediated immune suppression on human T cells. The higher blockade efficiency was observed for 2‐((3‐cyano‐4,6‐bis(4‐morpholinophenyl)pyridin‐2‐yl)thio)‐N‐(isoxazol‐3‐yl)acetamide (with total reversion at 100 μM) and methyl 2‐((3‐cyano‐4,6‐bis(4‐morpholinophenyl)pyridin‐2‐yl)thio)acetate (with partial reversion at 10 μM). Thus, this series of compounds illustrates a new chemotype of CD73 allosteric inhibitors.
Catalyst-Free Site Selective Hydroxyalkylation of 5-Phenylthiophen-2-amine with α-Trifluoromethyl Ketones through Electrophilic Aromatic Substitution Valentin Duvauchelle, David Bénimélis, Patrick Meffre, Zohra Benfodda Molecules, 2022 An original and effective approach for achieving trifluoromethyl hydroxyalkylation of 5-phenylthiophen-2-amine using α-trifluoromethyl ketones is described. In the last few years, reaction of Friedel-Crafts had been widely used to realize hydroxyalkylation on heterocycles such as indoles or thiophenes by means of Lewis acid as catalyst. Additionally, amine functions are rarely free when carbonyl reagents are used because of their tendency to form imines. This is the first time that a site-selective electrophilic aromatic substitution on C3 atom of an unprotected 5-phenylthiophen-2-amine moiety is reported. The liberty to allow reaction in neutral conditions between free amine is valuable in a synthesis pathway. The reaction proceeds smoothly using an atom-economical metal-and catalyst-free methodology in good to excellent yields. A mechanism similar to an electrophilic aromatic substitution has been proposed.
Synthesis, Structure Elucidation, Antibacterial Activities, and Synergistic Effects of Novel Juglone and Naphthazarin Derivatives Against Clinical Methicillin-Resistant Staphylococcus aureus Strains Valentin Duvauchelle, Chaimae Majdi, David Bénimélis, Catherine Dunyach-Remy, Patrick Meffre, et al. Frontiers in Chemistry, 2021 Infections caused by drug-resistant bacteria are a serious threat to human and global public health. Moreover, in recent years, very few antibiotics have been discovered and developed by pharmaceutical companies. Therefore, there is an urgent need to discover and develop new antibacterial agents to combat multidrug-resistant bacteria. In this study, two novel series of juglone/naphthazarin derivatives (43 compounds) were synthesized and evaluated for their antibacterial properties against various clinical and reference Gram-positive MSSA, clinical Gram-positive MRSA, and clinical and reference Gram-negative bacteria E. coli and P. aeruginosa. These strains are of clinical importance because they belong to ESKAPE pathogens. Compounds 3al, 5ag, and 3bg showed promising activity against clinical and reference MSSA (MIC: 1–8 µg/ml) and good efficacy against clinical MRSA (MIC: 2–8 µg/ml) strains. 5am and 3bm demonstrated better activity on both MSSA (MIC: 0.5 µg/ml) and MRSA (MIC: 2 µg/ml) strains. Their MICs were similar to those of cloxacillin against clinical MRSA strains. The synergistic effects of active compounds 3al, 5ag, 5am, 3bg, and 3bm were evaluated with reference antibiotics, and it was found that the antibiotic combination with 3bm efficiently enhanced the antimicrobial activity. Compound 3bm was found to restore the sensitivity of clinical MRSA to cloxacillin and enhanced the antibacterial activity of vancomycin when they were added together. In the presence of 3bm, the MIC values of vancomycin and cloxacillin were lowered up to 1/16th of the original MIC with an FIC index of 0.313. Moreover, compounds 3al, 5ag, 5am, 3bg, and 3bm did not present hemolytic activity on sheep red blood cells. In silico prediction of ADME profile parameter results for 3bm is promising and encouraging for further development.
Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes R Rajeshwari, V Duvauchelle, C Lindgren, K Stangner, S Knutsson, ... RSC Medicinal Chemistry , 2026 2026
Characterization of Alginates of Sargassum from the Archipelago of Guadeloupe N Marcin, V Thesnor, V Duvauchelle, A Ponce-Mora, L Gimeno-Mallench, ... Separations 11 (8), 226 , 2024 2024 Citations: 12
Investigation of PhoP Response Regulator inhibition to overcome resistance in Gram-negative clinical bacteria C Majdi, V Duvauchelle, M Seghir, D Bénimélis, C Dunyach-Rémy, ... International Journal of Antimicrobial Agents 64 (4), 107298 , 2024 2024
An overview on the antibacterial properties of juglone, naphthazarin, plumbagin and lawsone derivatives and their metal complexes C Majdi, V Duvauchelle, P Meffre, Z Benfodda Biomedicine & Pharmacotherapy 162, 114690 , 2023 2023 Citations: 50
Second‐generation CD73 inhibitors based on a 4, 6‐Biaryl‐2‐thiopyridine scaffold R Ghoteimi, A Braka, C Rodriguez, E Cros‐Perrial, V Duvauchelle, ... ChemMedChem 18 (7), e202200594 , 2023 2023 Citations: 13
Microwave-assisted synthesis of biodegradable and antibacterial thiophene, furan and thiazole derivatives M Rosales-Hurtado, V Duvauchelle, D Bénimélis, M Ogawa-Okada, ... Environmental Chemistry Letters 21 (1), 47-53 , 2023 2023 Citations: 12
Green methodologies for the synthesis of 2-aminothiophene V Duvauchelle, P Meffre, Z Benfodda Environmental Chemistry Letters 21 (1), 597-621 , 2023 2023 Citations: 35
Microwave-assisted synthesis of new environmentally friendly biodegradable and antibacterial heterocycles M Rosales-Hurtado, V Duvauchelle, D Bénimélis, M Ogawa-Okada, ... Environmental Chemistry Letters , 2022 2022
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery V Duvauchelle, P Meffre, Z Benfodda European Journal of Medicinal Chemistry 238, 114502 , 2022 2022 Citations: 40
Synergistic Effects of Novel Naphthoquinone Derivatives Against Clinical Methicilin-Resistant Staphylococcus aureus Strain V Duvauchelle, C Majdi, D Bénimélis, C Dunyach-Remy, P Meffre, ... REncontres en Chimie Organique Biologique 18 (RECOB18) , 2022 2022
Catalyst-free site selective hydroxyalkylation of 5-phenylthiophen-2-amine with α-trifluoromethyl ketones through electrophilic aromatic substitution V Duvauchelle, D Bénimélis, P Meffre, Z Benfodda Molecules 27 (3), 925 , 2022 2022 Citations: 2
Synthesis, structure elucidation, antibacterial activities, and synergistic effects of novel juglone and naphthazarin derivatives against clinical methicillin-resistant … V Duvauchelle, C Majdi, D Bénimélis, C Dunyach-Remy, P Meffre, ... Frontiers in Chemistry 9, 773981 , 2021 2021 Citations: 16
Evaluation of knowledge and risk perception about antibiotic resistance in biology and mathematics young students in Nîmes University in France V Duvauchelle, E Causse, J Michon, P Rateau, K Weiss, P Meffre, ... International Journal of Environmental Research and Public Health 18 (18), 9692 , 2021 2021 Citations: 4
Syntheses of juglone and naphtazarin novel derivatives and their antibacterial activities V Duvauchelle, Z Benfodda Semaine d'Etudes en Chimie Organique 57 (SECO57) , 2020 2020
Synthesis and biological evaluations of new families of histidine kinases inhibitors V Duvauchelle, M Rosales-Hurtado, T Boibessot, D Bénimèlis, ... GSO-JMJC-JED2019 , 2019 2019
MOST CITED SCHOLAR PUBLICATIONS
An overview on the antibacterial properties of juglone, naphthazarin, plumbagin and lawsone derivatives and their metal complexes C Majdi, V Duvauchelle, P Meffre, Z Benfodda Biomedicine & Pharmacotherapy 162, 114690 , 2023 2023 Citations: 50
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery V Duvauchelle, P Meffre, Z Benfodda European Journal of Medicinal Chemistry 238, 114502 , 2022 2022 Citations: 40
Green methodologies for the synthesis of 2-aminothiophene V Duvauchelle, P Meffre, Z Benfodda Environmental Chemistry Letters 21 (1), 597-621 , 2023 2023 Citations: 35
Synthesis, structure elucidation, antibacterial activities, and synergistic effects of novel juglone and naphthazarin derivatives against clinical methicillin-resistant … V Duvauchelle, C Majdi, D Bénimélis, C Dunyach-Remy, P Meffre, ... Frontiers in Chemistry 9, 773981 , 2021 2021 Citations: 16
Second‐generation CD73 inhibitors based on a 4, 6‐Biaryl‐2‐thiopyridine scaffold R Ghoteimi, A Braka, C Rodriguez, E Cros‐Perrial, V Duvauchelle, ... ChemMedChem 18 (7), e202200594 , 2023 2023 Citations: 13
Characterization of Alginates of Sargassum from the Archipelago of Guadeloupe N Marcin, V Thesnor, V Duvauchelle, A Ponce-Mora, L Gimeno-Mallench, ... Separations 11 (8), 226 , 2024 2024 Citations: 12
Microwave-assisted synthesis of biodegradable and antibacterial thiophene, furan and thiazole derivatives M Rosales-Hurtado, V Duvauchelle, D Bénimélis, M Ogawa-Okada, ... Environmental Chemistry Letters 21 (1), 47-53 , 2023 2023 Citations: 12
Evaluation of knowledge and risk perception about antibiotic resistance in biology and mathematics young students in Nîmes University in France V Duvauchelle, E Causse, J Michon, P Rateau, K Weiss, P Meffre, ... International Journal of Environmental Research and Public Health 18 (18), 9692 , 2021 2021 Citations: 4
Catalyst-free site selective hydroxyalkylation of 5-phenylthiophen-2-amine with α-trifluoromethyl ketones through electrophilic aromatic substitution V Duvauchelle, D Bénimélis, P Meffre, Z Benfodda Molecules 27 (3), 925 , 2022 2022 Citations: 2
Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes R Rajeshwari, V Duvauchelle, C Lindgren, K Stangner, S Knutsson, ... RSC Medicinal Chemistry , 2026 2026
Investigation of PhoP Response Regulator inhibition to overcome resistance in Gram-negative clinical bacteria C Majdi, V Duvauchelle, M Seghir, D Bénimélis, C Dunyach-Rémy, ... International Journal of Antimicrobial Agents 64 (4), 107298 , 2024 2024
Microwave-assisted synthesis of new environmentally friendly biodegradable and antibacterial heterocycles M Rosales-Hurtado, V Duvauchelle, D Bénimélis, M Ogawa-Okada, ... Environmental Chemistry Letters , 2022 2022
Synergistic Effects of Novel Naphthoquinone Derivatives Against Clinical Methicilin-Resistant Staphylococcus aureus Strain V Duvauchelle, C Majdi, D Bénimélis, C Dunyach-Remy, P Meffre, ... REncontres en Chimie Organique Biologique 18 (RECOB18) , 2022 2022
Syntheses of juglone and naphtazarin novel derivatives and their antibacterial activities V Duvauchelle, Z Benfodda Semaine d'Etudes en Chimie Organique 57 (SECO57) , 2020 2020
Synthesis and biological evaluations of new families of histidine kinases inhibitors V Duvauchelle, M Rosales-Hurtado, T Boibessot, D Bénimèlis, ... GSO-JMJC-JED2019 , 2019 2019