Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT(3) Receptor Ligands

[Image: see text] The 5-HT(3) receptor, a pentameric ligand-gated ion channel (pLGIC), is an important therapeutic target. During a recent fragment screen, 6-chloro-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine (1) was identified as a 5-HT(3)R hit fragment. Here we describe the synthesis...

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Autors principals: Verheij, Mark H. P., Thompson, Andrew J., van Muijlwijk-Koezen, Jacqueline E., Lummis, Sarah C. R., Leurs, Rob, de Esch, Iwan J. P.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2012
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3504484/
https://ncbi.nlm.nih.gov/pubmed/23006041
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300801u
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