Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors
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Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors. / Pinto, A; Tamborini, L; Mastronardi, F; Ettari, R; Safoz, Y; Bunch, Lennart; Nielsen, Birgitte; Jensen, Anders A.; De Micheli, C; Conti, P.
In: European Journal of Medicinal Chemistry, Vol. 75, 2014, p. 151-158.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors
AU - Pinto, A
AU - Tamborini, L
AU - Mastronardi, F
AU - Ettari, R
AU - Safoz, Y
AU - Bunch, Lennart
AU - Nielsen, Birgitte
AU - Jensen, Anders A.
AU - De Micheli, C
AU - Conti, P
PY - 2014
Y1 - 2014
N2 - Following the concept that increasing the molecular complexity may enhance the receptor selectivity, we replaced the 3-hydroxy-isoxazoline ring of model compound tricholomic acid with a 3-hydroxy-pyrazoline ring, which could be variously decorated at the N1 position, inserting groups characterized by different electronic and steric properties. Binding assays on rat brain synaptic membranes showed that, depending on the nature of the substituent, some of the new synthesized ligands interacted with either AMPA or KA receptors, with affinities in the mid-micromolar range.
AB - Following the concept that increasing the molecular complexity may enhance the receptor selectivity, we replaced the 3-hydroxy-isoxazoline ring of model compound tricholomic acid with a 3-hydroxy-pyrazoline ring, which could be variously decorated at the N1 position, inserting groups characterized by different electronic and steric properties. Binding assays on rat brain synaptic membranes showed that, depending on the nature of the substituent, some of the new synthesized ligands interacted with either AMPA or KA receptors, with affinities in the mid-micromolar range.
U2 - 10.1016/j.ejmech.2014.01.029
DO - 10.1016/j.ejmech.2014.01.029
M3 - Journal article
VL - 75
SP - 151
EP - 158
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -
ID: 98587296