Novel benzopolycyclic amines with NMDA receptor antagonist activity.
A new series of benzopolycyclic amines active as NMDA receptor antagonists were synthesized. Most of them exhibited increased activity compared with related analogues previously published. All the tested compounds were more potent than clinically approved amantadine and one of them displayed a lower IC50 value than memantine, an anti-Alzheimer's approved drug.
Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, s/n, Barcelona E-08028, Spain.
Elena
E
Valverde
Unitat de Farmacologia, Facultat de Medicina i Ciències de la Salut, Universitat Rovira i Virgili, c./St. Llorenç 21, Reus E-43201, Spain.
Francesc X
FX
Sureda
Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, s/n, Barcelona E-08028, Spain. Electronic address: svazquez@ub.edu.
Santiago
S
Vázquez
D000547:Amantadine / Q000737:chemistry / Q000378:metabolism; D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D008559:Memantine / Q000737:chemistry / Q000378:metabolism; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000588:Amines; D018696:Neuroprotective Agents; D016194:Receptors, N-Methyl-D-Aspartate; D000547:Amantadine; D008559:Memantine
Amantadine; Memantine; NMDA; Polycyclic compounds; Prins–Ritter reaction