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CARBORANES --- LIGANDS --- CARBORANES --- LIGANDS

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Proteins --- Ligands --- Congresses.

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This book contains an overview of complex formation by macrocyclic ligand systems. The study of macrocyclic chemistry represents a major area of activity which impinges on a range of other areas in both chemistry and biochemistry. The field has characteristically yielded many interesting and unusual compounds. The text discusses the structures and properties of macrocyclic compounds; the synthesis of macrocycles; polyether crown and related systems; metal-ion and molecular recognition (host-guest chemistry); as well as kinetic, thermodynamic and electrochemical aspects of a range of macrocyclic systems. A discussion of the different categories of naturally occurring macrocycles is also included. Specialist and non-specialist alike will find this a useful text. Apart from serving as a convenient reference for established workers in the field, it should also prove useful to new graduate students as well as to researchers from other areas who seek a general introduction to the subject. The topics discussed also provide a suitable basis for a senior undergraduate or graduate course in macrocyclic chemistry and inorganic complexes.

Ligands. --- Macrocyclic compounds.

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Coordination compounds --- Chemical bonds --- Ligands

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The G protein-coupled receptor GPR 119 has recently been described as the receptor of the bioactive lipid oleoylethanolamide (N-oleoylethanolamine, OEA). This lipid is known for its anorexigenic properties, in the same time the GPR l 19 receptor has been involved in the regulation of glucose metabolism. The few ligands described so far for GPR l 19 led us to develop a research project to synthesize a library of potential ligands for this receptor. One of the ligands described in the literature is built around a 1,2,4-oxadiazole scaffold, therefore our choice of guide structure has focused on 1,2,4-oxadiazoles-type derivatives substituted in position 3 and 5. The synthetic pathways leading to thi s chemical series have been explored to facilitate the synthesis. Thus, we have developed a magnesia-supported microwave-enhanced reaction. This method uses no solvent and benefits from the microwave to activate the reactions and can be regarded as "green chemistry". It allowed us to synthesize several series of compounds by varying the nature of substituents in position 3 and 5. On the other hand, to increase the structural diversity we conducted preliminary testing for the synthesis of 1.2,4- thiadiazoles, that are sulfur isosters of 1,2,4-oxadiazoles. Le récepteur couplé aux protéines G GPR 119 a récemment été décrit comme le récepteur du lipide bioactif oléoyléthanolamide (N-oléoyléthanolamine, OEA). Ce lipide est connu pour ses propriétés anorexigènes, et d'autre part, le récepteur GPR 119 semble impliqué dans la régulation du métabolisme glucidique. Le peu de ligands décrits à ce jour pour ce récepteur nous a poussés à développer un projet ayant pour objet la synthèse d'une bibliothèque de ligands potentiels de ce récepteur. Un des ligands décrits dans la littérature possédant un noyau 1,2,4-oxadiazole, notre choix de structure guide s'est porté sur des dérivés de type 1,2,4-oxadiazole substitués en position 3 et 5. Les voies d'accès vers cette série chimique ont été explorées en vue d'en faciliter la synthèse. Nous avons ainsi développé une méthode de synthèse en phase solide utilisant les micro-ondes. Cette méthode n'utilisant pas de solvant et bénéficiant des micro-ondes pour activer les réactions peut être considérée comme étant de la « green chemistry », ou chimie verte. Cette méthode nous a permis de synthétiser plusieurs séries de composés variant par la nature des substituants en position 3 et 5. D'autre part, en vue d'augmenter la diversité structurale nous avons mené des essais préliminaires de synthèse de 1,2,4-thiadiazoles, isostères soufrés des 1,2,4-oxadiazoles.

GPR119 protein, human --- Ligands --- Endocannabinoids