Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists
复制标题
DOI：
10.1016/j.ejmech.2016.03.016
复制
发表时间：
2016-06-10
影响因子：
6.7
通讯作者：
Zhang, Lihe
中科院分区：
文献类型：
--
作者：
Xue, Yu;Tang, Jingshu;Zhang, Lihe
人α 7烟碱型乙酰胆碱受体（nAChR）是治疗精神分裂症伴认知功能障碍的一个很有前途的治疗靶点。在此，我们报告了一系列靶向α 7 nAChR的中氮茚衍生物的合成和激动活性。结果显示，所有合成的化合物对α 7 nAChR具有亲和力，并且一些化合物产生强激动活性，特别是大多数活性激动剂显示出比对照EVP-6124更高的效力。对接和构效关系研究为开发更有效的新型α 7 nAChR激动剂提供了见解。(C)2016 Elsevier Masson SAS。All rights reserved.
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.