TY - JOUR
T1 - Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity
AU - Karig, G
AU - Large, J M
AU - Sharples, C G V
AU - Sutherland, A
AU - Gallagher, T
AU - Wonnacott, S
PY - 2003/9/1
Y1 - 2003/9/1
N2 - 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.
AB - 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.
UR - http://dx.doi.org/10.1016/s0960-894x(03)00594-8
U2 - 10.1016/s0960-894x(03)00594-8
DO - 10.1016/s0960-894x(03)00594-8
M3 - Article
SN - 0960-894X
VL - 13
SP - 2825
EP - 2828
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
IS - 17
ER -