| Title | Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists |
| Authors | Xue, Yu Tang, Jingshu Ma, Xiaozhuo Li, Qing Xie, Bingxue Hao, Yuchen Jin, Hongwei Wang, Kewei Zhang, Guisen Zhang, Liangren Zhang, Lihe |
| Affiliation | Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China. Peking Univ, PKU IDG McGovern Inst Brain Res, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China. Jiangsu Nhwa Pharmaceut Co Ltd, 69 Minzhu South Rd, Xuzhou 227116, Jiangsu, Peoples R China. Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China. Wang, KW (reprint author), Peking Univ, PKU IDG McGovern Inst Brain Res, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China. |
| Keywords | alpha 7 nAChR Indolizine Agonists SAR Schizophrenia NICOTINIC ACETYLCHOLINE-RECEPTOR BAYLIS-HILLMAN REACTION CENTRAL-NERVOUS-SYSTEM LIGAND-BINDING DOMAIN PHARMACOLOGICAL CHARACTERIZATION SUBUNIT GENE SCHIZOPHRENIA DISCOVERY INHIBITORS DISORDERS |
| Issue Date | 2016 |
| Publisher | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY |
| Citation | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.2016,115,94-108. |
| Abstract | Human alpha 7 nicotinic acetylcholine receptor (nAChR) is a promising therapeutic target for the treatment of schizophrenia accompanied with cognitive impairment. Herein, we report the synthesis and agonistic activities of a series of indolizine derivatives targeting to alpha 7 nAChR. The results show that all synthesized compounds have affinity to alpha 7 nAChR and some give strong agonistic activity, particularly most active agonists show higher potency than control EVP-6124. The docking and structure-activity relationship studies provide insights to develop more potent novel alpha 7 nAChR agonists. (C) 2016 Elsevier Masson SAS. All rights reserved. |
| URI | http://hdl.handle.net/20.500.11897/434445 |
| ISSN | 0223-5234 |
| DOI | 10.1016/j.ejmech.2016.03.016 |
| Indexed | SCI(E) PubMed |
| Appears in Collections: | 药学院 天然药物与仿生药物国家重点实验室 |
