Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1358734 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
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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Related Topics
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Chemistry
Organic Chemistry
Authors
Xinxian Deng, Lin Guo, Lili Xu, Xuechu Zhen, Kunqian Yu, Weili Zhao, Wei Fu,