Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs

Camps, Pelayo; Duque, Maria D.; Vazquez, Santiago; Naesens, Lieve; De Clercq, Erik; Sureda, Francesc X.; Lopez-Querol, Marta; Camins, Antoni; Pallas, Merce; Prathalingam, S. Radhika; Kelly, John M.; Romero, Vanessa; Ivorra, Dolores; Cortes, Diego

Abstract

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.

Más información

Título según WOS: ID WOS:000260927000005 Not found in local WOS DB
Título de la Revista: BIOORGANIC & MEDICINAL CHEMISTRY
Volumen: 16
Número: 23
Editorial: PERGAMON-ELSEVIER SCIENCE LTD
Fecha de publicación: 2008
Página de inicio: 9925
Página final: 9936
DOI:

10.1016/j.bmc.2008.10.028

Notas: ISI