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Syntheses and Biological Properties of Pyrido[3,4‐ b ]homotropane (PHT) and its Analogues with Bridged Aza‐[ n .2.1] Skeletons
Author(s) -
Sun Bingxia,
Wang Zhongwen
Publication year - 2019
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.201900348
Subject(s) - chemistry , nonane , stereochemistry , nicotinic acetylcholine receptor , biological activity , molecule , acetylcholine receptor , combinatorial chemistry , receptor , biochemistry , organic chemistry , in vitro
The nicotinic acetylcholine receptor (nAChR) is one of the targets for developing drugs for the treatment of central nervous system (CNS) disorders and for control of agricultural pests. Pyrido[3,4‐ b ] homotropane (PHT) was originally designed and synthesized by Kanne and co‐workers and showed strong affinity binding to nAChR. PHT has a novel aza‐[4.2.1]nonane skeleton. Owing to its excellent biological activities and novel chemical structure, synthetic and medicinal chemists have been attracted by this molecule. Some PHT analogues with bridged aza‐[n.2.1] skeletons were also designed and synthesized via different strategies. Herein, we summarize the syntheses of PHT and its analogues. Their biological activity study is also briefly discussed.