Medicinal Chemistry - URA CNRS 2128  

  HEADDr.Yves L. Janin /
  MEMBERSDr. Sandrine Guillou (Post-doc); Dr. Nicolas Wlodarczyk (post-doc); Anne Noel (M2 student)

  Annual Report

Our work focusses on the following projects.

- A collaboration with the Paris Descartes University and Stewart Cole (Ecole Polytechnique de Lausanne) aimed at studying the structure-activity relationship of an original series of specific antimycobacterial compounds created through original chemistry. However, the biological activity of the compounds created was not sufficiently high to be exploited.

- Starting from an unexpectedly efficient access to alkoxypyrazoles, we set to prepare and evaluate whole arrays of new chemical entities. This project, sponsored by the “Pole de Compétitivité Medicen”, aimed at preparing original building blocks and chemical libraries followed by their biological assessment against infectious diseases, by the screening platform managed by Hélène Munier-Lehman. From the chemistry point of view, the results led us to patent and publish many original aspects of pyrazole chemistry, including building blocks such as the one depicted in the following scheme. Studies on the antimicrobial activity of these compounds will be the subject of further research.

Keywords: Medicinal Chemistry, Building Blocks, Tuberculosis, Malaria, New Chemical Entities



- Janin, Y.L. 2007, Antituberculosis drugs: ten years of research. Bioorg. Med. Chem, 15, 2479-2513. PMID: 17291770

- Guillou, S.; Bonhomme, F.J.; Janin, Y.L. 2008, An improved preparation of 3-alkoxypyrazoles. Synthesis, 3504-3508. PMID: 20333718

- Janin, Y.L. 2010, ATPase inhibitors of heat shock protein 90, second season. Drug Discov. Today, 15, 342-353. PMID: 20230904

- Guillou, S.; Janin, Y.L. 2010, 5-Iodo-3-ethoxypyrazoles, an entry point to new chemical entities. Chem. Eur. J., 16, 4669-4677.

- Guillou, S.; Bonhomme, F.J.; Chahine, D.; Nesme, O.; Janin, Y.L. 2010, N-arylation of 3-alkoxypyrazoles, the case of the pyridines. Tetrahedron, 66, 2654-2663.

Activity Reports 2010 - Institut Pasteur
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