New oxapolycyclic cage amines with NMDA receptor antagonist and trypanocidal activities

Several benzopolycyclic amines have been synthesized and their NMDA receptor antagonist and trypanocidal activities have been studied. Four of them displayed similar activity to memantine as NMDA receptor antagonists and several derivatives showed a significant level of trypanocidal activity. The sy...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2010, Vol.18 (1), p.46-57
Hauptverfasser:	Duque, María D., Camps, Pelayo, Torres, Eva, Valverde, Elena, Sureda, Francesc X., López-Querol, Marta, Camins, Antoni, Prathalingam, S. Radhika, Kelly, John M., Vázquez, Santiago
Format:	Artikel
Sprache:	eng
Schlagworte:	Amantadine Amines - chemical synthesis Amines - chemistry Amines - pharmacology Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Antiparkinson Agents - chemical synthesis Antiparkinson Agents - chemistry Antiparkinson Agents - pharmacology Biological and medical sciences Cells, Cultured Humans Indantadol Medical sciences Memantine Memantine - pharmacology Molecular Structure Neurons - drug effects NGP1-01 NMDA Parkinson Disease - drug therapy Pharmacology. Drug treatments Polycyclic cage compounds Rats Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - metabolism Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma Trypanosoma brucei brucei - drug effects Trypanosomiasis - drug therapy
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Zusammenfassung:	Several benzopolycyclic amines have been synthesized and their NMDA receptor antagonist and trypanocidal activities have been studied. Four of them displayed similar activity to memantine as NMDA receptor antagonists and several derivatives showed a significant level of trypanocidal activity. The synthesis of several (1,2,3,5,6,7-hexahydro-1,5:3,7-dimethano-4-benzoxonin-3-yl)amines and related compounds is reported. Several of them display very similar activity to memantine as NMDA receptor antagonists. Several derivatives showed a significant level of trypanocidal activity.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.11.017