A5062538597- Tuberculosis Research and Epidemiology
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Biochemical and Molecular Research
- Cancer therapeutics and mechanisms
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- Sphingolipid Metabolism and Signaling
- Click Chemistry and Applications
- Lipid Membrane Structure and Behavior
- DNA and Nucleic Acid Chemistry
- Lysosomal Storage Disorders Research
- Drug Solubulity and Delivery Systems
- Mycobacterium research and diagnosis
- Advanced biosensing and bioanalysis techniques
- Analytical Methods in Pharmaceuticals
- Bone Tissue Engineering Materials
- Enzyme function and inhibition
- Synthesis and Biological Evaluation
- RNA and protein synthesis mechanisms
- Spectroscopy and Quantum Chemical Studies
- Bioactive Compounds and Antitumor Agents
- African Botany and Ecology Studies
- Periodontal Regeneration and Treatments
- Microbial Natural Products and Biosynthesis
Université Toulouse III - Paul Sabatier
2012-2025
Molécules d'Intérêt Biologique
2013-2024
Centre National de la Recherche Scientifique
2013-2024
Université de Toulouse
2010-2021
Pharmacochimie et Pharmacologie pour le Développement
2003
Institut de Biochimie et Génétique Cellulaires
1994-1995
<title>Abstract</title> In respiratory airway epithelial cells lipopolysaccharide (LPS) treatment induced an enhancement of connexin 26 (Cx26) hemichannel activity shown by dye uptake experiments combined with siRNA knock-down Cx26. This effect was already observed at infection relevant concentrations (≤ 10 ng/mL LPS) and involved tumor necrosis factor (TNF)-α- Ca<sup>2+</sup>-dependent signaling. High (1 µg/mL reduced the transepithelial electrical resistance (TEER) Calu-3 35 % within...
InhA, an NAD‐dependent enoyl‐acyl carrier protein reductase, is involved in the biosynthesis of mycolic acids, specific lipids to mycobacteria. InhA target isoniazid, a first‐line anti‐tuberculosis drug used since 1950s. Isoniazid prodrug that needs be activated by catalase‐peroxidase KatG. Due resistance problems, substantial amount work has been carried out identify or design direct inhibitors demonstrating this enzyme still considered relevant for discovery new drugs. Much included...
Tuberculosis is a serious public health problem worldwide. The search for new antibiotics has become priority, especially with the emergence of resistant strains. A family imidazoquinoline derivatives, structurally analogous to triazolophthalazines, which had previously shown good antituberculosis activity, were designed inhibit InhA, an essential enzyme Mycobacterium tuberculosis survival. Over twenty molecules synthesized and results showed modest inhibitory efficacy against protein....
Constrained nucleic acids (α,β-D-CNAs) have an ethylene bridge that locks the α and β backbone torsion angles of DNA in canonical (gauche(−),trans) conformation, as B-form (see picture), or noncanonical (gauche(+),trans) conformation. Canonical α,β-D-CNAs enhance duplex-forming ability oligonucleotides with complementary DNA, while stabilize distorted B-DNA structures. Supporting information for this article is available on WWW under...
In this work, two classes of Carbonic Anhydrase (CA) inhibitors, sulfonamide and coumarin derivatives linked to pyta moiety (2a-b) their corresponding rhenium complexes (3a-b), were designed. These compounds synthesized fully characterized by classical analytical methods X-ray diffraction. All the evaluated for inhibitory activity against hCA isoforms I, II, IX XII. They exhibited high activities in range nanomolar both XII isoforms. The compound 2a showed strongest inhibition...
Konformativ eingeschränkte Nucleinsäuren (α,β-D-CNAs) enthalten eine Ethylenbrücke, die Rückgratwinkel α und β einer DNA in der kanonischen (gauche(−),trans) oder nichtkanonischen Konformation (gauche(+), trans) arretiert. Kanonische α,β-D-CNAs verstärken Duplexbildung von Oligonucleotiden mit komplementärer DNA, während nichtkanonische verzerrte B-DNA-Strukturen stabilisieren. Supporting information for this article is available on the WWW under...
A series of 12 analogues the Cer transfer protein (CERT) antagonist HPA-12 with long aliphatic chains were prepared as their (1R,3S)-syn and (1R,3R)-anti stereoisomers from pivotal chiral oxoamino acids. The enantioselective access to these intermediates well ensuing transformation relied on a practical crystallization-induced asymmetric (CIAT) process. Sonogashira coupling followed by triple bond reduction thiophene ring hydrodesulfurization (HDS) into corresponding alkane moieties was then...