Novel benzopolycyclic amines with NMDA receptor antagonist activity

• Published in: Bioorganic & medicinal chemistry Vol. 22; no. 9; pp. 2678 - 2683
• Main Authors: Valverde, Elena, Sureda, Francesc X., Vázquez, Santiago
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 01.05.2014; Elsevier
• Subjects: Amantadine; Amantadine - chemistry; Amantadine - metabolism; Amines - chemical synthesis; Amines - chemistry; Amines - metabolism; Biochemistry & Molecular Biology; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Life Sciences & Biomedicine; Memantine; Memantine - chemistry; Memantine - metabolism; Neuroprotective Agents - chemical synthesis; Neuroprotective Agents - chemistry; Neuroprotective Agents - metabolism; NMDA; Pharmacology & Pharmacy; Physical Sciences; Polycyclic compounds; Prins–Ritter reaction; Protein Binding; Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors; Receptors, N-Methyl-D-Aspartate - metabolism; Science & Technology; NMDA; Amantadine; Memantine; Prins–Ritter reaction; Polycyclic compounds; Prins-Ritter reaction; ALZHEIMERS-DISEASE; SELECTIVE NMDA; PHARMACOLOGICAL EVALUATION
• ISSN: 0968-0896; 1464-3391; 1464-3391
• DOI: 10.1016/j.bmc.2014.03.025

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.