Littérature scientifique sur le sujet « Inhibiteurs directs »
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Articles de revues sur le sujet "Inhibiteurs directs"
Lecompte, T., M. Toussaint-Hacquard et J. Devignes. « Les anticoagulants inhibiteurs directs de la thrombine ». Annales Françaises d'Anesthésie et de Réanimation 28, no 9 (septembre 2009) : S3—S7. http://dx.doi.org/10.1016/s0750-7658(09)72458-x.
Texte intégralA. EKOU. « AOD et fibrillation atriale ». Les pathologies vasculaires (anciennement ANGEIOLOGIE) 71, no 03 (1 septembre 2019) : 8. http://dx.doi.org/10.54695/mva.71.03.2228.
Texte intégralMeddahi, S., et M. M. Samama. « Les inhibiteurs directs de la thrombine, l’hirudine, la bivalirudine, l’argatroban, et le dabigatran etexilate ». Journal des Maladies Vasculaires 36, no 1 (février 2011) : 24–32. http://dx.doi.org/10.1016/j.jmv.2010.11.005.
Texte intégralMeddahi, S., et M. M. Samama. « Caractéristiques pharmacologiques et cliniques des inhibiteurs directs du facteur Xa : rivaroxaban, apixaban, edoxaban et betrixaban ». Journal des Maladies Vasculaires 39, no 3 (mai 2014) : 183–94. http://dx.doi.org/10.1016/j.jmv.2014.02.001.
Texte intégralFernandez, Dr Eugenio, et Pr Martine Louis Simonet. « Y a-t-il une [b]place[/b] aujourd’hui pour les inhibiteurs directs de la rénine ? » Revue Médicale Suisse 6, no 267 (2010) : 1963–67. http://dx.doi.org/10.53738/revmed.2010.6.267.1963.
Texte intégralChappell, Neena L., Carren Dujela et André Smith. « Spouse and Adult Child Differences in Caregiving Burden ». Canadian Journal on Aging / La Revue canadienne du vieillissement 33, no 4 (23 septembre 2014) : 462–72. http://dx.doi.org/10.1017/s0714980814000336.
Texte intégralMargelidon-Cozzolino, V., S. Hodin, X. Delavenne et L. Bertoletti. « Étude des interactions médicamenteuses entre anticoagulants oraux directs et inhibiteurs de la phosphodiestérase de type-5 : y-a-t-il un risque pour les patients atteints d’hypertension artérielle pulmonaire ? » Revue des Maladies Respiratoires 35 (janvier 2018) : A148—A149. http://dx.doi.org/10.1016/j.rmr.2017.10.326.
Texte intégralJ.-M. M. « Innovation : premier inhibiteur direct de la rénine plasmatique ». Revue Francophone des Laboratoires 2006, no 383 (juin 2006) : 10. http://dx.doi.org/10.1016/s1773-035x(06)80206-6.
Texte intégralGnädinger, Lukas C., Michael Gagesch et Martin Schimmel. « Relations entre le bruxisme et les troubles neurocognitifs ». SWISS DENTAL JOURNAL SSO – Science and Clinical Topics 127, no 12 (11 décembre 2017) : 1086–92. http://dx.doi.org/10.61872/sdj-2017-12-04.
Texte intégralCouic-Marinier, Françoise. « Ordonnance contenant un inhibiteur direct de la thrombine, chez un patient en fibrillation atriale permanente ». Actualités Pharmaceutiques 52, no 525 (avril 2013) : 13–16. http://dx.doi.org/10.1016/j.actpha.2013.02.003.
Texte intégralThèses sur le sujet "Inhibiteurs directs"
Tamhaev, Rasoul. « Conception, synthèse et caractérisation de dérivés diaryl éthers comme nouveaux inhibiteurs directs de la protéine InhA de Mycobacterium tuberculosis ». Electronic Thesis or Diss., Université de Toulouse (2023-....), 2024. http://thesesups.ups-tlse.fr/6088/.
Texte intégralTuberculosis, despite being a very ancient disease, remains one of the major causes of mortality due to a single infectious agent. In 2021, 10 million people contracted the disease and 1.5 million deaths were directly attributable to it. Despite the availability of a variety of antibiotics, few of them prove effective against the pathogen responsible for tuberculosis, Mycobacterium tuberculosis. This ineffectiveness is primarily due to the impermeable nature of the mycobacterial cell envelope, composed mainly of mycolic acids. Isoniazid, the most widely used first-line antitubercular drug, targets the biosynthesis of these mycolic acids through the protein InhA. Isoniazid acts as a pro-drug requiring activation by the protein KatG. However, the emergence of resistance during the activation stage of isoniazid necessitates the development of direct inhibitors of InhA. The work carried out during this thesis aimed to develop new direct inhibitors of InhA. These inhibitors were designed basedon the structure of a diaryl ether motif, known for its ability to inhibit the enzyme. Dynamic combinatorial chemistry combined with X-ray crystallography was used as a fragment screening method to discover new inhibitors. Three adducts, visualized directly within the active site of the protein, were characterized and showed interactions with the major portal of the protein. In another project, a new family of diaryl ethers with three pharmacophores was designed to fully occupy the substrate binding site. One of the synthesized molecules exhibited sub-micromolar inhibitory activity against InhA. The structure of the corresponding complex was resolved by X-ray crystallography, highlighting a wider opening of one of the protein's regions, called the minor portal. Finally, multi-target approaches, targeting both InhA and the dehydratase complex HadABC of the FAS II system, were also developed during this thesis. Several dual molecules were produced, showing inhibition of InhA activity in the nanomolar range. These molecules also demonstrated inhibition of the growth of different mycobacterial strains
Bailly, François. « Optimisation du traitement anti-VHC : place des dosages pharmacologiques et des cinétiques virales à l'ère des antiviraux directs ». Thesis, Lyon 1, 2013. http://www.theses.fr/2013LYO10328/document.
Texte intégralThe rapid development of new direct antiviral agents (DAA) against HCV gives hope of more potent and well tolerated treatments. These new compounds will deeply modify therapeutic schedules, virological response prognostic factors and patients’ monitoring. The aim of our work was to define the relevance of ribavirin plasma concentration and viral kinetics monitoring during triple therapy. The study of a prospective cohort including 186 patients under triple therapy showed an SVR12 rate of 60%. Associated predictive factors were IL-28B genotype and previous treatment response. A reversible decrease of glomerular filtration rate was also observed. Ribavirin plasma concentration monitoring reduced hematological risks among patients with renal insufficiency. Early ribavirin plasma exposure showed an underexposure among HIV/HCV patients and ribavirin biodisponibility with severe anemia increased among telaprevir-treated patients. Within the CUPIC cohort, the initial viral load undetectability or decrease up to 50% or 70% at week 2 of triple therapy were predictive of SVR12. Moreover, this week 2 viral load assessment allowed the detection of early viral breakthrough. Ribavirin still plays a major role in current and future therapeutic strategies. Ribavirin monitoring could also be important during future multi-drug therapy that could be associated with drug interactions
Le, Bescont Julie. « Inhibiteurs photo-contrôlables de la famille TAM - Méthodologie de sulfénylation directe d'imidazopyridines ». Thesis, université Paris-Saclay, 2020. http://www.theses.fr/2020UPASF016.
Texte intégralThe TAM family consists in 3 tyrosine kinases : Tyro3, Axl and Mer. These proteins are involved in many cellular processes and pathways. The TAM family has been identified as a new promising target for cancer therapy, autoimmune diseases and viral infections. However, only a few inhibitors have been developped for this family. The first chapter of this manuscript is dedicated to the conception, synthesis and biological evaluation of new inhibitors for the TAM family. To bypass the maindrawback of protein kinase inhibitors, selectivity, we chose to apply the concept of photopharmacology. This strategy enable spatial and temporal control of the drug activity upon irradiation. By blocking a key position of the inhibitor with a photoremovable group, we can inactivate the molecule, and restore the activity upon irradiation. We introduced different photoremovable protecting groups on our inhibitors. The choice of the groups, the synthesis, the photo-cleavage and the biological evaluation will be discussed in chapter 2.Finally, we also developped a methodology for direct sulfenylation of imidazopyridines using DABCO.(SO₂)₂ as sulfur source
Besselièvre, François. « Arylation, alcénylation et alcynylation directes d'azoles et conception et synthèse d'inhibiteurs de la polymérase du virus de la dengue ». Paris 11, 2010. http://www.theses.fr/2010PA112008.
Texte intégralThe dengue is a mosquito-borne viral disease. Every year, 500 000 persons are being hospitalized because of this disease and 25 000 die from severe infections. The mosquito is found in subtropical area where 2,5 billion people live. Nearly half the population of the earth is at risk of beinf infected. Today, there is absolutely no treatment nor vaccination available. To fight against the disease molecules inhibiting the multiplication of the virus are required. The viral polymerase NS5 is very important for this replication and is an excellent target for drug development. Dr Canard group in Marseille has studied the polymerase for years and has designed a test in order to screen libraries of compound an find inhibitors of NS5. Therefore, the Curie/CNRS library (>10000 molecules) has been screened and 3 molecules called “hits” have shown interesting activities. The aim of this work was to develop modern chemistry that allows the rapid production of analogs of those 3 hits. To this end. Palladium and copper catalysed direct arylation, alkenylation and alkynylation of azole have been carried out. Many molecules were synthesized and some of them gave interesting results on the isolated polymerase but also in infested cells
Rouvre, Ingrid. « Hydrogénase - Promoteur ou inhibiteur de la corrosion microbienne ? » Phd thesis, Toulouse, INPT, 2016. http://oatao.univ-toulouse.fr/16482/1/Rouvre_Ingrid.pdf.
Texte intégralMoulin, Paccaly Anne J. « Approches pharmacocinétiques/pharmacodynamiques appliquées au développement d'un nouvel inhibiteur direct du facteur Xa pour le traitement de la thrombose artérielle ». Paris 5, 2005. http://www.theses.fr/2005PA05P630.
Texte intégralOtamixaban, is a novel direct FXa inhibitor for the treatment of arterial thrombosis. This clinical pharmacology work aims the study of the pharmacokinetic (PK) and pharmacodynamic (PD) properties of otamixaban as well as the development of modeling and simulations (M&S) to support the Phase II/III studies using data in healthy subjects and in chronic coronary patients. A “fingerprint of PK/PD markers for anticoagulant effect” was generated, including the measurements of anti-FXa activity, of clotting times (aPTT, PT, dPT, RVVT et HCT) and of the inhibition of thrombin generation. The non-dose proportional pharmacokinetics of otamixaban was investigated and built into the pharmacokinetic models. The lack of a major gender and age effect on the PK and PD parameters was demonstrated. Finally, the absence of any drug-drug interactions and the complementarities of the anticoagulant effect of OTAM and of the anti-platelet effects of modifiers of the platelet function has been reported for tirofiban and acetyl salicylic acid
Rouchon, Dagois Myriam. « Synthèse d'analogues de la Télomestatine, stabilisants de G-quadruplexes et potentiellement inhibiteurs de la télomérase ». Paris 11, 2008. http://www.theses.fr/2008PA112210.
Texte intégralTelomere is a section of DNA with a single-stranded overlap located at the extremities of the chromosomes and composed of repeating sequences (TTAGGG)n in humans. During each cell division, a number of base pairs is lost until a critical telomere length is reached. In cancer cells, the enzyme telomerase is over-expressed and allows telomere length to be maintained. The subsequent lack of critical limits leads to anarchic proliferation of immortal cancer cells. The guanine-rich telomere DNA can fold upon itself to form a quadruplex conformer and such a structure may be stabilized with certain small-molecule ligand. Telomestatin is currently the most active known ligand but its recently reported total synthesis requires more than 30 steps. We proposed to prepare heterocyclic analogues of telomestatin in order to analyze their biological properties. After differents preliminary studies, oligopyridyloxazole were synthetised by direct arylation. To macrocylise the hepta-aryle compound with two terminal oxazoles, studies of oxazole dimerisation were studied. Among all the prepared analogues, one of them has interesting properties. For more complete understanding, differents physico-chemical studies has been done: UV-visible and fluorimetric titrations, FID, circular dichroism. In collaboration with the equip of Jean-Louis Mergny (Muséum National d’Histoires Naturelles), FRET-melting test and test of binding-POT1 has been also studied
Baladi, Tom. « Autour du noyau imidazo[4,5-b]pyridine : inhibiteurs potentiels de la protéine kinase Tyro3 et fonctionnalisation directe de liaisons C – H ». Thesis, Université Paris-Saclay (ComUE), 2016. http://www.theses.fr/2016SACLS386/document.
Texte intégralBladder cancer is a major medical issue, being the fourth most frequent cancer in men and treatable only with heavy surgery and/or broad-spectrum chemotherapy. This thesis project deals with the discovery of new targeted therapies of bladder cancer by blocking specifically, at a molecular scale in cancer cells, the signaling pathways in which protein kinase Tyro3 is involved. Indeed, its overexpression in most bladder cancers and the major part it plays in cancer cells survival have led to the validation of protein kinase Tyro3 as a therapeutic target for the treatment of bladder cancer. This thesis project can be divided into three main parts: the development of new synthetic methods around the imidazo[4,5-b]pyridine scaffold, the synthesis of a library of compounds using these methods and eventually the study of structure-activity relationships of these compounds versus Tyro3
Moussaoui, Myriam. « Relations structure-fonction-dynamique des flavohémoglobines de bactéries pathogènes et non pathogènes ». Thesis, Université Paris-Saclay (ComUE), 2016. http://www.theses.fr/2016SACLS034.
Texte intégralFor some pathogens, flavohemoglobins (FlavoHbs) play an important role in the defense of microorganisms by conferring them a resistance against nitrosative stress generated by the immune system cells. Since these protein are absent in human, several studies have been conducted in order to understand the functioning of these proteins at the molecular level, considering them as potential attractive targets for selective inhibitors. Their inactivation results a loss of virulence. Chemical compounds such as azole derivatives have been identified as being capable of inhibiting their enzymatic function and thereby affecting the bacterial virulence factors. If these compounds are widely used in the treatment of invasive fungal skin infections, their potential antibacterial activity is not yet operated.Typically, flavoHbs are composed of three domains: an N-terminal globin domain which harbors a single heme b and a C-terminal ferredoxin reductase-like FAD- and NAD-binding module. The crystallographic structures of flavoHbs show that these proteins are able to adopt different conformations depending on the nature and the presence of heme ligand but also depending on different organisms they are coming from. The different conformations are characterized by a rigid body motion of one of the three domains. We have undertaken in this work, the study of the Staphyloccocus aureus flavoHb, poorly studied in the literature, and compared it to the Ralstonia eutropha flavoHb (non pathogenic bacteria) to provide new and more specific information on behaviors of these proteins derived from pathogens.This PhD work describes first the functional and biochemical characterization of the S. aureus flavoHb. Due to the lack of its crystallographic structure, a theoretical structural model was designed based on the strong sequence homology between the amino acid sequence of S. aureus and Saccharomyces cerevisiae for which the 3D structure was recently determined. We hypothesized that the relative movement of protein domains could be a way to regulate its enzymatic activity by controlling the substrate accessibility. The Phe396 residue (nomenclature according to R. eutropha), suggested by the structural data to play an important role in the enzyme functioning, but also in the equilibrium between different conformations, was substituted by the Ala or Serine amino acids. The effects of the punctual mutations were investigated with respect to the enzyme functioning and biochemical properties. The mutations effect on the internal electron transfer between flavoHbs cofactors (heme and FAD) was also studied by spectroscopic techniques. This work showed that the impact of Phe substitution on the enzymatic properties is different, depending the considered flavoHb and revealed an additional binding site for other substrate than the native one. The effects of azole derivative inhibitors and also quinones and nitroaromatic compounds have been studied on native and genetically modified enzymes functioning. The latter compounds may act as the ‘subversive substrates’ for flavoHb, converting its protective functions into the cytotoxic ones.Taken as a whole, this work showed that, although the protein structures and sequences are similar, the flavoHbs from different bacteria may behave differently towards an identical mutation, an identical inhibitor and could display different catalytic cycles
Casse, Céline. « Etude de l'activation paradoxale de la transcription a partir du promoteur du ltr-vih-1 par les inhibiteurs de la transcription ». Paris 5, 2001. http://www.theses.fr/2001PA05S001.
Texte intégralChapitres de livres sur le sujet "Inhibiteurs directs"
MONTESINOS, Emilio, Esther BADOSA, Maria PLA, Laura MONTESINOS et Anna BONATERRA. « Peptides antimicrobiens et éliciteurs de défense pour lutter contre les maladies végétales ». Dans Biocontrôle des maladies des plantes, 127–66. ISTE Group, 2024. http://dx.doi.org/10.51926/iste.9098.ch6.
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