Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity

Reference:

Karig, G., Large, J. M., Sharples, C. G. V., Sutherland, A., Gallagher, T. and Wonnacott, S., 2003. Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity. Bioorganic & Medicinal Chemistry Letters, 13 (17), pp. 2825-2828.

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Official URL:

http://dx.doi.org/10.1016/s0960-894x(03)00594-8

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 a7 selectivity as compared to UB-165 and deschloro UB-165 2. These results are discussed within the context of recent pharmacophore models.

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