Academic Journal
Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds.
| العنوان: | Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds. |
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| المؤلفون: | Charton, Julie, Charruault, Lise, Déprez-Poulain, Rebecca, Déprez, Benoit |
| المساهمون: | Biostructures et Decouverte de Medicament, Institut Pasteur de Lille, Pasteur Network (Réseau International des Instituts Pasteur)-Pasteur Network (Réseau International des Instituts Pasteur)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille, Droit et Santé, We are grateful to the institutions that support our laboratory (Inserm, Université de Lille2 and Institut Pasteur de Lille). Data management was performed using Pipeline Pilot™ from Scitegic. We thank also the following institutions or companies: CAMPLP and VARIAN. inc.This project was supported by the European Commission -ERDF funds, grant N° OBJ2 –2006/364.1 N°302. |
| المصدر: | ISSN: 1386-2073 ; Combinatorial Chemistry and High Throughput Screening ; https://inserm.hal.science/inserm-00281198 ; Combinatorial Chemistry and High Throughput Screening, 2008, 11 (4), pp.294-303. ⟨10.2174/138620708784246013⟩. |
| بيانات النشر: | CCSD Bentham Science Publishers |
| سنة النشر: | 2008 |
| المجموعة: | Réseau International des Instituts Pasteur, Paris: HAL-RIIP |
| مصطلحات موضوعية: | MESH: Amines/chemical synthesis, MESH: Amines/chemistry, MESH: Chelating Agents/chemical synthesis, MESH: Chelating Agents/chemistry, MESH: Chemistry, Pharmaceutical/methods, MESH: Combinatorial Chemistry Techniques/methods, MESH: Cyclobutanes/chemistry, MESH: Enzyme Inhibitors/chemical synthesis, MESH: Enzyme Inhibitors/chemistry, MESH: Esters/chemistry, MESH: Hydroxamic Acids/chemistry, MESH: Molecular Structure, MESH: Pharmaceutical Preparations/chemical synthesis, MESH: Pharmaceutical Preparations/chemistry, MESH: Piperidines/chemistry, MESH: Small Molecule Libraries/chemical synthesis, MESH: Small Molecule Libraries/chemistry, MESH: Zinc/chemistry, [SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences |
| الوصف: | International audience ; Many natural privileged scaffolds contain a basic nitrogen atom, which often is a key element of pharmacophore and a chemically reactive centre as well. In our ongoing research program devoted to the design of targeted libraries based on acidic templates, we developed methods to convert privileged basic compounds -like natural alkaloids or drugs into acidic compounds. This conversion led to a profound alteration of the pharmacophore, without changing the overall shape and lipophilicity of the molecule. We expect such modifications to generate unexpected biological activities. Recently, we focused on derivatives of squaric acid, a vinylogous carboxylic acid. Two series were studied. First we describe a new, selective parallel synthesis of squaramic acids from a dissymmetric diester (3-tert-butoxy-4-ethoxy-cyclobut-3-en-1,2-dione). This efficient procedure avoids the synthesis of the undesired squaramides. Secondly we describe a microplate parallel synthesis (15 micromol-scale) of squaric acid hydroxamate amides from a squaric hydroxamate ester. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| Relation: | info:eu-repo/semantics/altIdentifier/pmid/18473739; PUBMED: 18473739 |
| DOI: | 10.2174/138620708784246013 |
| الاتاحة: | https://inserm.hal.science/inserm-00281198 https://inserm.hal.science/inserm-00281198v1/document https://inserm.hal.science/inserm-00281198v1/file/CCHTS-Charton_et_al.pdf https://doi.org/10.2174/138620708784246013 |
| Rights: | info:eu-repo/semantics/OpenAccess |
| رقم الانضمام: | edsbas.82EE639 |
| قاعدة البيانات: | BASE |
| DOI: | 10.2174/138620708784246013 |
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