2. Academic Validation
  3. Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold

Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold

  • Bioorg Med Chem Lett. 2015 Sep 15;25(18):3970-4. doi: 10.1016/j.bmcl.2015.07.030.
Xinxian Deng 1,  Lin Guo 2,  Lili Xu 1,  Xuechu Zhen 3,  Kunqian Yu 2,  Weili Zhao 4,  Wei Fu 5
Affiliations

Affiliations

  • 1 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.
  • 2 Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 3 Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-disorders & Department of Pharmacology, College of Pharmaceutical Sciences, Soochow University, 199 Ren'ai Road, Suzhou, Jiangsu Province 215123, China. Electronic address: zhenxuechu@suda.edu.cn.
  • 4 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. Electronic address: zhaoweili@fudan.edu.cn.
  • 5 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. Electronic address: wfu@fudan.edu.cn.
PMID: 26227779 DOI: 10.1016/j.bmcl.2015.07.030
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.

Keywords

5-HT(2A) receptor antagonist; Molecular docking; Quinazoline derivatives; Synthesis.

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