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In-situ Synthese von selektiven Antagonisten für unterschiedliche Typen von nikotinischen Acetylcholin-Rezeptoren mit allylischen Aziden als Triazol-Vorstufen

English title Achieving Selectivity for Nicotinic Receptors Subtype Antagonists by Using an in situ Click-Chemistry Approach with Allylic Azides as Triazole Precursors.
Applicant Stump Bernhard
Number 118872
Funding scheme Fellowships for prospective researchers
Research institution The Skaggs Institute for Chemical Biology The Scripps Research Institute
Institution of higher education Institution abroad - IACH
Main discipline Organic Chemistry
Start/End 01.09.2007 - 31.08.2008
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Keywords (3)

in-situ click chemistry; nicotinic acetylcholine receptor antagonists; allylic azides

Lay Summary (English)

Lead
Lay summary
The aim of the proposed project is to apply the in situ click chemistry approach to find potent ligands that are able to distinguish between subtypes of ligand gated ion channels. As model systems for those channels, acetylcholine binding proteins of three different organisms have been chosen.Nicotinic Acetylcholine Receptors are prototypes for the pharmaceutically important family of pentameric ligand-gated ion channels. The nicotinic Acetylcholine Receptors themselves are involved in pathological conditions such as Alzheimer`s disease, Parkinson`s disease, some forms of epilepsy, depression, autism and schizophrenia. They are also the targets of tobacco-smoking effects and addiction, rendering antagonists to have potential value in ablation of the addicitive actions of nicotine.The in situ click chemistry approach will be extended for the first time to allylic azides. These triazole precursors enable more connection possibilities out of a single precursor combination, thus broadening the structural diversity of theoretically accessible combinations from smaller azide/alkyne libraries.The proposed work will be carried out in the group of Prof. K. B. Sharpless at the Scripps Research Institute.
Direct link to Lay Summary Last update: 21.02.2013

Responsible applicant and co-applicants

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