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

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.