Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs
作者:Pelayo Camps、María D. Duque、Santiago Vázquez、Lieve Naesens、Erik De Clercq、Francesc X. Sureda、Marta López-Querol、Antoni Camins、Mercè Pallàs、S. Radhika Prathalingam、John M. Kelly、Vanessa Romero、Dolores Ivorra、Diego Cortés
DOI:10.1016/j.bmc.2008.10.028
日期:2008.12
The synthesis of several (3-noradamantyl)amines, [(3-noradamantyl)methyl]amines, (3,7-dimethyl-1-bisnoradamantyl)amines, and [(3,7-dimethyl-1-bisnoradamantyl)methyl]amines is reported. They were evaluated against a wide range of viruses and one of them inhibited the cytopathicity of influenza A virus at a concentration similar to that of amantadine. Several of the new polycyclic amines show an interesting activity as NMDA receptor antagonists. A rimantadine analogue displayed significant trypanocidal activity. Moreover, to further characterize the pharmacology of these compounds, their effects on dopamine uptake were also assessed. (c) 2008 Elsevier Ltd. All rights reserved.