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N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators

Thewlis, Kevin M., Aldegheri, Laura, Harries, Mark H., Mookherjee, Claudette, Oliosi, Beatrice and Ward, Simon 2010. N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators. Bioorganic & Medicinal Chemistry Letters 20 (23) , pp. 7116-7119. 10.1016/j.bmcl.2010.09.062

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A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Uncontrolled Keywords: AMPA, Receptor, Modulators, Synthesis
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 10 September 2010
Last Modified: 21 Feb 2018 11:01

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