Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT3 Receptor Ligands

…, AJ Thompson, JE van Muijlwijk-Koezen…

Index: Verheij, Mark H. P.; Thompson, Andrew J.; Van Muijlwijk-Koezen, Jacqueline E.; Lummis, Sarah C. R.; Leurs, Rob; De Esch, Iwan J. P. Journal of Medicinal Chemistry, 2012 , vol. 55, # 20 p. 8603 - 8614

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Citation Number: 17

Abstract

The 5-HT3 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-HT3R hit fragment. Here we describe the synthesis and structure–activity relationships (SAR) of a series of (iso) quinoline and quinazoline compounds that were synthesized and screened for 5-HT3R ...