Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371791 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the α7 neuronal nicotinic receptor (Ki = 56 nM). 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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Related Topics
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Chemistry
Organic Chemistry
Authors
Michael R. Schrimpf, Kevin B. Sippy, Clark A. Briggs, David J. Anderson, Tao Li, Jianguo Ji, Jennifer M. Frost, Carol S. Surowy, William H. Bunnelle, Murali Gopalakrishnan, Michael D. Meyer,