A5029979249- Malaria Research and Control
- Pneumocystis jirovecii pneumonia detection and treatment
- Antibiotic Resistance in Bacteria
- Tuberculosis Research and Epidemiology
- HIV/AIDS drug development and treatment
- Synthesis of β-Lactam Compounds
- Computational Drug Discovery Methods
- Synthesis and Catalytic Reactions
- Immune Cell Function and Interaction
- Antibiotic Use and Resistance
- Phenothiazines and Benzothiazines Synthesis and Activities
- Research on Leishmaniasis Studies
- Drug-Induced Hepatotoxicity and Protection
- RNA modifications and cancer
- Microplastics and Plastic Pollution
- Organic and Inorganic Chemical Reactions
- Historical and Environmental Studies
- T-cell and B-cell Immunology
- Drug Transport and Resistance Mechanisms
- Bioactive Compounds and Antitumor Agents
- Click Chemistry and Applications
- Peptidase Inhibition and Analysis
- Microbial Natural Products and Biosynthesis
- Healthcare Systems and Practices
- Chemical Reaction Mechanisms
Centre National de la Recherche Scientifique
2003-2024
Université de Montpellier
2006-2024
Laboratoire HydroSciences Montpellier
2022-2024
Institut de Recherche pour le Développement
2024
Centre Hospitalier Universitaire de Montpellier
2022-2024
Institut des Biomolécules Max Mousseron
2008-2023
École Nationale Supérieure de Chimie de Montpellier
2020-2023
Laboratoire de Chimie Organique
2004
Herein, we describe a new methodology for selective cephalosporin functionalization at the C3 position. First an optimization study reaction conditions is performed and allowed to define favorable parameters...
Metallo-β-lactamases (MBLs) contribute to the resistance of Gram-negative bacteria carbapenems, last-resort antibiotics at hospital, and MBL inhibitors are urgently needed preserve these important antibacterial drugs. Here, we describe a series 1,2,4-triazole-3-thione-based displaying an α-amino acid substituent, which amine was mono- or disubstituted by (hetero)aryl groups. Compounds certain nitrogen-containing heterocycles showed submicromolar activities against VIM-type enzymes strong...
Abstract Metallo‐β‐lactamases (MBLs) are increasingly involved as a major mechanism of resistance to carbapenems in relevant opportunistic Gram‐negative pathogens. Unfortunately, clinically efficient MBL inhibitors still represent an unmet medical need. We previously reported several series compounds based on the 1,2,4‐triazole‐3‐thione scaffold. In particular, Schiff bases formed between diversely 5‐substituted‐4‐amino and 2‐carboxybenzaldehyde were broad‐spectrum VIM‐type, NDM‐1 IMP‐1...
Abstract Natural killer T (NKT) cells are a distinct subset of mature lymphocytes endowed with features activated and regulatory cells. α ‐Galactosylceramides ( ‐GalCers), the synthetic prototype which is KRN7000, only natural reagents recognised by T‐cell receptor NKT The α‐GalCer‐activated promptly release IFN γ IL‐4 (IFN=interferon; IL=interleukin) undergo apoptotic death within hours. In mice, responsible for antitumour activity protection against autoimmune diseases. KRN7000 can thus be...
Addressing antibacterial resistance is a major concern of the modern world. The development new approaches to meet this deadly threat critical priority. In article, we investigate approach negate bacterial resistance: exploit β-lactam bond cleavage by β-lactamases selectively trigger prodrugs into periplasm. Indeed, multidrug-resistant Gram-negative pathogens commonly produce several that are able inactivate antibiotics, our most reliable and widely used therapeutic option. chemical...
Abstract Plasmodium falciparum is responsible of the most severe form malaria, and new targets novel chemotherapeutic scaffolds are needed to fight emerging multidrug‐resistant strains this parasite. Bis‐alkylguanidines have been designed mimic choline, resulting in inhibition plasmodial de novo phosphatidylcholine biosynthesis. Despite potent vitro antiplasmodial vivo antimalarial activities, a major drawback these compounds for further clinical development their low oral bioavailability....
Resistance is futile: A new series of hybrid bis-cations has been synthesized as potent antimalarial agents. These compounds have two different cationic heads derived from bisthiazolium and bisamidine salts. Structure–activity relationships data suggest that the nature linker plays a critical role in activity, leading to with significant oral activity against Plasmodium parasites. Detailed facts importance specialist readers are published "Supporting Information". Such documents...
Abstract The main threat to controlling malaria is the emerging multidrug resistance of Plasmodium sp. parasites. Bis‐alkylamidines were developed as a potential new chemotherapy that targets plasmodial phospholipid metabolism. Unfortunately, these compounds are not orally available. To solve this absorption issue, we investigated prodrug strategy based on sulfonate derivatives alkylamidoximes. A total 25 sulfonates synthesized candidates one bis‐ N ‐alkylamidine and six N‐substituted C...
Head and neck squamous cell carcinoma (HNSCC) is one of the leading causes cancer-related deaths calls for new druggable targets. We have previously highlighted critical role ADP-ribosylation factor-1 (Arf1) activation in HNSCC. In present study, we address question whether targeting Arf1 could be proposed as a valuable strategy against HNSCC.We rationally designed synthesized constrained ATC-based (4-amino-(methyl)-1,3-thiazole-5-carboxylic acid) γ-dipeptides to block activation. evaluated...
Based on the Buchwald–Hartwig amination reaction, an original β-lactam pronucleosides series was synthesized and microbiologically evaluated.
Abstract ADP-ribosylation factor 1 (Arf1) is a crucial regulator in vesicle-mediated membrane trafficking and involved the activation of signaling molecules. However, molecular mechanisms underlying Arf1-dependent cancer development progression are far from understood. We report here that Arf1 most amplified gene Arf family breast cancer, knocking it down leads to an induction autophagy via AMPK pathway. To effectively target Arf1, we rationally designed synthesized constrained ATC-based...
Abstract NDM-1 (New-Delhi-Metallo-β-lactamase-1) is an enzyme developed by bacteria that implicated in resistance to almost all known antibiotics. In this study, we deliver a new, curated bioactivities database, along with set of unifying rules for managing different activity properties and inconsistencies. We define the classification problem terms Multiple Instance Learning, employing embeddings corresponding molecular substructures present ensemble ranking framework, relaying on k-fold...