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SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
22
Issue
4
Identifiers
DOI: 10.1016/j.bmcl.2011.12.126
Keywords
  • α7 Neuronal Nicotinic Receptor
  • Nachr
  • Nnr
  • Agonist
  • Tilorone
  • Fluorenone
  • Xanthenone
  • Mitsunobu

Abstract

Abstract The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the α7 neuronal nicotinic receptor (Ki=56nM). SAR investigations determined that both basic sidechains are essential for potent activity, however active monosubstituted derivatives can also be prepared if the flexible sidechains are replaced with conformationally rigidified cyclic amines. Analogs in which the fluorenone core is replaced with either dibenzothiophene-5,5-dioxide or xanthenone also retain potent activity.

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