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Protein-protein interactions (PPIs) constitute many potential therapeutic targets for the discovery of new drugs. Given their specificity, PPIs are more challenging to target than other ligands. Thus, finding the best screening process can be difficult. Moreover, PPIs often have no direct accessible activity readout. Therefore, it can be unclear which test to choose for the screening of small molecules targeting PPIs. Given that noncellular assays are the most suitable both as first screening assays and for high-throughput screening (HTS), here we focus on noncellular screening assays. For each assay, we discuss the principles and advantages/drawbacks and provide a recent example. We also highlight the crucial parameters to take into account to select the most suitable assays to screen PPI modulators.

International audience; Herein we describe the drug design steps developed to increase the radical scavenging and β-amyloid aggregation inhibitory activities of a previously described series of benzylidenephenylpyrrolizinones. Among the newly synthesized derivatives, some benzylphenylpyrrolizinones exhibited interesting results in regard to those activities. Initial druggability parameters were measured, and suggest these compounds as a suitable starting point for potential alternatives in treating Alzheimer's disease

Performing Jefford’s cyclization of ethyl 2-pyrrol-1-ylcyclohex-2-ene-1-carboxylate (5) using boron tribromide in refluxing dichloromethane led to a trans–cis bromopyrrolohydrindolone 7 whose debromination in alkaline medium afforded a highly strained cyclopenta[1,3]cyclopropa[1,2-b]pyrrolizin-8-one 6. Compound 7 and two of its diastereoisomers were synthesized in order to better understand this unusual reaction and more generally the reactivity of these systems.

With the increase of life expectancy, age-related macular degeneration has become a major public health problem to which the community pharmacist is able to provide solutions. In this thesis, a survey was conducted giving us an overview of the amount of information available to patients with an exudative form of AMD. In turn we could channel what role the pharmacist has in the treatment process. Thus, we will be discussing his role in disease prevention and detection as well as how he can help with care and support for patients with AMD.; Avec l’augmentation de l’espérance de vie, la dégénérescence maculaire liée à l’âge est devenue un problème majeur de santé publique auquel le pharmacien d’officine est capable d’apporter des solutions. Dans ce travail, la réalisation d’un questionnaire a permis de faire un état des lieux sur le niveau d’information des patients atteints par une forme exsudative de DMLA dans le but de dégager les principaux axes de réflexion concernant la place du pharmacien d’officine dans le parcours de soin. Ainsi, il sera question de son rôle dans la prévention et le dépistage de la maladie mais également dans la prise en charge et l’accompagnement du patient atteint de DMLA.

Since their commercialization in 1963, benzodiazepines have been widely prescribed. Having many uses (anxiolytic, hypnotic, muscle relaxant and antiseizure drug), a large proportion of the population have consumed it during their lifetime. But their undesirable effects, such as dependence, paradoxical reactions or anterograde amnesia, led to an important misuse of these molecules. In this thesis, we will confront the use of benzodiazepines in France and Vietnam, in relation to the mentality and the philosophy of the populations.; Depuis leur arrivée sur le marché en 1963, les benzodiazépines ont largement été prescrites. Possédant de nombreuses utilisations (anxiolytique, hypnotique, myorelaxante et anti-convulsivante), une large proportion de la population en ont consommé durant leur vie. Mais leurs effets indésirables, tels que la dépendance, les réactions paradoxales ou encore l’amnésie antérograde, ont conduit à un mésusage important de ces molécules. Dans cette thèse, nous confronterons l’utilisation des benzodiazépines en France et au Vietnam, en relation avec la mentalité et la philosophie des populations étudiées.