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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
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.
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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem