| Title : Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity - Karig_2003_Bioorg.Med.Chem.Lett_13_2825 |
| Author(s) : Karig G , Large JM , Sharples CG , Sutherland A , Gallagher T , Wonnacott S |
| Ref : Bioorganic & Medicinal Chemistry Lett , 13 :2825 , 2003 |
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Abstract :
Four racemic phenyl-substituted analogues 3-6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the alpha(4)beta(2), alpha(3)beta(4), and alpha(7) neuronal nicotinic receptors. The 2'-phenyl derivative 3 shows no activity at these major receptor subtypes, while the 4'-phenyl analogue 4 shows an enhanced level of alpha(7) selectivity as compared to UB-165 and deschloro UB-165 2. These results are discussed within the context of recent pharmacophore models. |
| PubMedSearch : Karig_2003_Bioorg.Med.Chem.Lett_13_2825 |
| PubMedID: 14611837 |
Karig G, Large JM, Sharples CG, Sutherland A, Gallagher T, Wonnacott S (2003)
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity
Bioorganic & Medicinal Chemistry Lett
13 :2825
Karig G, Large JM, Sharples CG, Sutherland A, Gallagher T, Wonnacott S (2003)
Bioorganic & Medicinal Chemistry Lett
13 :2825