Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines

Several (2-oxaadamant-1-yl)amines have been synthesized and their antiviral, NMDA receptor antagonist, and trypanocidal activities have been studied. The synthesis of several (2-oxaadamant-1-yl)amines is reported. They were evaluated as NMDA receptor antagonists and several of them were more active...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2009-04, Vol.17 (8), p.3198-3206
Hauptverfasser:	Duque, María D., Camps, Pelayo, Profire, Lenuta, Montaner, Silvia, Vázquez, Santiago, Sureda, Francesc X., Mallol, Jordi, López-Querol, Marta, Naesens, Lieve, Clercq, Erik De, Radhika Prathalingam, S., Kelly, John M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Adamantane Adamantane - analogs & derivatives Adamantane - chemical synthesis Adamantane - pharmacology Amantadine Amines - chemical synthesis Amines - pharmacology Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Biological and medical sciences Cage compounds Cell Culture Techniques Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences Memantine Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NGP1-01 NMDA Pharmacology. Drug treatments Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - metabolism Trypanocidal Agents - chemical synthesis Trypanocidal Agents - pharmacology Trypanosoma
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Zusammenfassung:	Several (2-oxaadamant-1-yl)amines have been synthesized and their antiviral, NMDA receptor antagonist, and trypanocidal activities have been studied. The synthesis of several (2-oxaadamant-1-yl)amines is reported. They were evaluated as NMDA receptor antagonists and several of them were more active than amantadine, but none was more potent than memantine. None of the tested compounds displayed antiviral activity. Two of the derivatives showed a significant level of trypanocidal activity.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.02.007