Article ID Journal Published Year Pages File Type
1358734 Bioorganic & Medicinal Chemistry Letters 2015 5 Pages PDF
Abstract

A series of compounds with quinazoline scaffold were designed, synthesized and evaluated as novel potent 5-HT2A receptor ligands. N-(4-Chlorophenyl)-2-(piperazin-1-yl)quinazolin-4-amine (5o) has a Ki value of 14.04 ± 0.21 nM, with a selectivity more than 10,000 fold over 5-HT1A receptors (D1 and D2-like receptors). The functional assay showed that this compound is an antagonist to 5-HT2A receptor with an IC50 value of 1.66 μM.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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