926649-64-1Relevant articles and documents
Synthesis of 3-hydroxy- and 3-carboxy-Δ2-isoxazoline amino acids and evaluation of their interaction with GABA receptors and transporters
Conti, Paola,De Amici, Marco,Pinto, Andrea,Tamborini, Lucia,Grazioso, Giovanni,Frolund, Bente,Nielsen, Birgitte,Thomsen, Christian,Ebert, Bjarke,De Micheli, Carlo
, p. 5533 - 5542 (2006)
A series of 3-hydroxy- and 3-carboxy-Δ2-isoxazoline amino acids, structurally related to the GABAA agonist THIP and to the GABA uptake inhibitors THPO and exo-THPO, was prepared by means of synthetic strategies involving the 1,3-dipolar cycloaddition of nitrile oxides. All derivatives were submitted to a pharmacological investigation at both GABA receptors and transporters. Unfortunately, all amino acids were devoid of activity except for a very low affinity at GABAA receptors, displayed by compounds 8 and 17. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.