Synthesis of benzopolycyclic cage amines: NMDA receptor antagonist, trypanocidal and antiviral activities.

Eva Torres; María D Duque; Marta López-Querol; Martin C Taylor ORCID logo; Lieve Naesens; Chunlong Ma; Lawrence H Pinto; Francesc X Sureda; John M Kelly ORCID logo; Santiago Vázquez; (2012) Synthesis of benzopolycyclic cage amines: NMDA receptor antagonist, trypanocidal and antiviral activities. Bioorganic & medicinal chemistry, 20 (2). pp. 942-948. ISSN 0968-0896 DOI: 10.1016/j.bmc.2011.11.050
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The synthesis of several 6,7,8,9,10,11-hexahydro-9-methyl-5,7:9,11-dimethano-5H-benzocyclononen-7-amines is reported. Several of them display low micromolar NMDA receptor antagonist and/or trypanocidal activities. Two compounds are endowed with micromolar anti vesicular stomatitis virus activity, while only one compound shows micromolar anti-influenza activity. The anti-influenza activity of this compound does not seem to be mediated by blocking of the M2 protein.

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