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Design and synthesis of bridged piperidine and piperazine isosteres
Gaëtan Maertens1, Oscar M Saavedra1, Vito Vece1
1Department of Chemistry, Université de Montréal, Station Centre-Ville, C.P. 6128 Montréal, QC H3C 3J7, Canada.
Bioorganic & Medicinal Chemistry Letters
|June 26, 2018
Abstract:
We have developed versatile methods toward the synthesis of a variety of piperidine/piperazine bridged isosteres of pridopidine. The compounds were assessed against the D2 receptor in agonist and antagonist modes and against the D4 receptor in agonist mode. hERG Binding and the ADME profiles were studied.
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