Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.

Abstract

Human α7 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 α7 nAChR. The results show that all synthesized compounds have affinity to α7 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 α7 nAChR agonists.

• Authors: Yu Xue, Jingshu Tang, Xiaozhuo Ma, Qing Li, Bingxue Xie, Yuchen Hao, Hongwei Jin, Kewei Wang, Guisen Zhang, Liangren Zhang, Lihe Zhang
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 115 Pg. 94-108 (Jun 10 2016) ISSN: 1768-3254 [Electronic] France
• PMID: 26994846 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Chemical References

• Indolizines
• alpha7 Nicotinic Acetylcholine Receptor
• indolizine

Topics

• Dose-Response Relationship, Drug
• Humans
• Indolizines (chemical synthesis, chemistry, pharmacology)
• Molecular Docking Simulation
• Molecular Structure
• Structure-Activity Relationship
• alpha7 Nicotinic Acetylcholine Receptor (agonists)