Deng Xinxian, Guo Lin, Xu Lili, Zhen Xuechu, Yu Kunqian, Zhao Weili, Fu Wei
Department of Medicinal Chemistry & Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Bioorg Med Chem Lett. 2015 Sep 15;25(18):3970-4. doi: 10.1016/j.bmcl.2015.07.030. Epub 2015 Jul 18.
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.
设计、合成并评估了一系列具有喹唑啉骨架的化合物，作为新型强效5-HT2A受体配体。N-(4-氯苯基)-2-(哌嗪-1-基)喹唑啉-4-胺(5o)的Ki值为14.04±0.21 nM，对5-HT1A受体（D1和D2样受体）的选择性超过10000倍。功能试验表明，该化合物是一种5-HT2A受体拮抗剂，IC50值为1.66 μM。
