Littérature scientifique sur le sujet « Synthèse (chimie) – Inhibiteurs »
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Articles de revues sur le sujet "Synthèse (chimie) – Inhibiteurs"
Agbodan, Kokou Agbékonyi, Oudjaniyobi Simalou, Gneiny Whad Tchani et Koffi Jondo. « Etude de l’influence de la basicité sur l’enthalpie de réaction des sels N-méthoxycarbonyl-(oxy)-pyridiniums ». International Journal of Biological and Chemical Sciences 14, no 4 (17 août 2020) : 1489–98. http://dx.doi.org/10.4314/ijbcs.v14i4.26.
Texte intégralThèses sur le sujet "Synthèse (chimie) – Inhibiteurs"
Balg, Christian. « Synthèse d'inhibiteurs des aminoacyl-ARNt synthétases et des aminoacyl-ARNt amidotransférases ». Thesis, Université Laval, 2011. http://www.theses.ulaval.ca/2011/28241/28241.pdf.
Texte intégralBaumann, Jean Sébastien. « Synthèse de glyconanostructures : inhibiteurs potentiels des interactions sucres-protéines ». Amiens, 2011. http://www.theses.fr/2011AMIE0102.
Texte intégralThe central theme of this thesis is the design and synthesis of diverse family of “multivalent” glyconanostructures as potential inhibitors of glycosyltransferases and glycosylhydrolases. A special emphasis is placed on ppGalNAcTs because of their role in the biosynthesis of O-glycans (mucins). A library of multivalent macromolecules has been targeted based on the supposed mode-of-action of these enzymes. The targeted glycostructures are comprised of various scaffolds (fullerenes, nanodiamonds, boron-doped diamonds, polymers…) and various glycan mimics/iminosugars. New strategies based on dominos reactions have been developed to obtain the iminosugar components. Each of the various fragments have been functionalised with either azido or alkyne groups and then combined employing a 1,3 dipolar cycloaddition reaction. Several members of the targeted glyconanostructure library have been obtained. The successful synthesis of these new glyconano sructures has allowed to probe how weak interactions typically observed between glycans and their biological receptors manifest themselves in the case of little-studied catalytic proteins such as the ppGalNAcTs. The types of glyconanostructures synthesized in this work have great potential as tools in the domain of glycomics which is attracting a good deal of attention at the present time
Xu, Bixue. « Synthèse de Mono- et gem-Difluoro-Carba-glycosides ». Paris 6, 2012. http://www.theses.fr/2012PA066305.
Texte intégralCarbasugars, as hydrolytically stable carbohydrate mimetics in which endocyclic oxygen atom has been replaced by a methylene group, have attracted great interest among chemists and biochemists due to their potential biological properties, particularly as inhibitors of glycosidase or glycosyltransferases. However, the replacement of the endocyclic oxygen by a methylene group has the inherent disadvantage to suppress any possible hydrogen bonding as well as exo-anomeric effect, an important factor in directing the relative positioning between two monosaccharide residues. One way to overcome this problem is to replace the endocyclic oxygen atom by gem-difluoromethylene group (-CF2-) which would hopefully induce conformational bias through stereoelectronic effects to partially restore the exo-anomeric effect as well as provide key polar region for the interaction with potential receptors. In this work, we successfully realized the first syntheses of mono- and gem-difluoro- carba-glycoside analogues of mono- and disaccharides. Our strategy is based on a Lewis acid induced carbocyclization of glycosides of an enolether possessing an electron-donating group with retention of the anomeric group. Two strategies for the synthesis of mono- and gem-difluoro-carbaglycosides were established as illustrated in the retrosynthetic plan Figure 1. They differentiate by the stage of introduction of fluorine atom: before or after the carbocyclization step
Abdo, Marie-Rose. « Synthèses et activités d'agent antibrucelliens : inhibiteurs de l'histidinol déshydrogénase ». Montpellier 2, 2007. http://www.theses.fr/2007MON20107.
Texte intégralLeclercq, Julien. « Conception, synthèse et évaluation pharmacologique de nouveaux inhibiteurs de la kinésine Eg5 ». Thesis, Lille 2, 2014. http://www.theses.fr/2014LIL2S026/document.
Texte intégralCancer is a real problem in our civilization. Indeed, in 2010, it affected more than 10 million people in the world. Today, this disease is the first cause of death in industrialized countries.Unfortunately, the proposed therapies remain frequently insufficient and lead to side effects which remove the benefits of the medical treatment. In order to avoid the toxicity to safe cells, since a few years, researches have been done to develop targeted therapies. Most of the anti-mitotic drugs actually available on the market lead to important side effects such as cardiological, hematological and neurotoxic problems.Thus, we interested to another therapeutic target which still acts at the level of the mitosis but causing fewer side effects and can be overexpressed into the cancer cells: the mitotic kinesin Eg5.The mitotic kinesin Eg5 plays an important role in the early stages of mitosis and is one of the most attractive target enzymes in antimitotic drug development. The modulation of the Eg5 activity has been shown to cause aberrant mitotic spindle formation, cell cycle arrest during mitosis and the inhibition of proliferation of tumor cells in culture. With regard to the potential of Eg5 modulators in the treatment of human cancers, we report the design, synthesis and biological studies of quinazolinone derivatives as mitotic kinesin Eg5 inhibitors. We developed three series of molecules derived from quinazolin-4-one scaffold following a “de novo drug design” strategy
Gessier, Vincent. « Synthèse, ex pool chiral, d'imidazolo-sucres, inhibiteurs de glycosidases et de glycosyltransférases ». Mulhouse, 2001. http://www.theses.fr/2001MULH0657.
Texte intégralChabaud, Laurent. « Carboazidation d'allylsilanes chiraux : application à la synthèse totale d'alcaloïdes polyhydroxyles inhibiteurs de glycosidases ». Bordeaux 1, 2005. http://www.theses.fr/2005BOR13040.
Texte intégralLoidreau, Yvonnick. « Synthèse de composés hétérocycliques [6,5,6] polyhétéroatomiques, inhibiteurs potentiels de kinases ». Rouen, 2013. http://www.theses.fr/2013ROUES001.
Texte intégralIn this manuscript, we describe the design, synthesis and potential applications of a combinatorial library based on polyheteroatomic [6,5,6] planar tricyclic structure. Initially, a study of different synthetic ways to bicyclic [6,5] precursors was carried out. Upon completion of these scaffolds, the third heterocycle was generated by using decomposition of formamide or from the Dimroth rearrangement. More than one hundred molecules were obtained following this work. The products of this library were screened on seven families of kinases (CDK-5, GSK-3, CK-1, DYRK-1A, CK-1, EGF-R and VEGF-R) in order to determine a lead compound 87 (0. 031 nM on CK-1 and 0. 68 microM on CLK-1). A last study consisted in modulating this compound by Suzuki cross-coupling. Finally, more than two hundred molecules were synthetized and this project opens various pharmacological perspectives
Haddoub, Rose. « Synthèse des aloisines immobilisées ». Lyon 1, 2006. http://www.theses.fr/2006LYO10299.
Texte intégralRecent results have shown that aloisine A (7-nButyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b] pyrazine) is a potent inhibitor of CDK. An original methodology aiming at identifying potential secondary inhibition targets relies on the immobilization of the inhibitor on solid matrix, followed by identification of proteins with high affinity for the inhibitor by affinity chromatography of a cellular extract. To this end, both aloisine A and the negative control N-methyl aloisine bearing extended linker chain have been synthesized. We present here the preparation of the new aloisine analogues bearing a triethylene glycol chain at different positions of the molecule, terminated by an amine suitable for the immobilisation on an agarose-based matrix. Furthemore, we show that conjugation of the molecule with the linker via a cycloaddition [3+2] allows efficient coupling to the matrix as well as access to aloisine derivatives conjugated with biologically relevent molecules such as biotine, or a tyrosine residue targeting LAT1 for transport of drugs through the blood-brain barrier
Oulaïdi, Farah. « Conception et synthèse d'iminoglycolipides comme inhibiteurs d'enzymes lysosomales à effet chaperon pharmacologique ». Phd thesis, Université d'Orléans, 2011. http://tel.archives-ouvertes.fr/tel-00623109.
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