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Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents

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dc.contributor.author Joubert, Jacques
dc.contributor.author Malan, Sarel Francois
dc.contributor.author Van Dyk, Sandra
dc.contributor.author Green, Ivan R.
dc.date.accessioned 2012-09-11T10:50:13Z
dc.date.available 2012-09-11T10:50:13Z
dc.date.issued 2011
dc.identifier.citation Joubert, J. et al. 2011. Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents. Bioorganic & medicinal chemistry, 19(13):3935-3944. [http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry/] en_US
dc.identifier.issn 0968-0896
dc.identifier.issn 1464-3391 (Online)
dc.identifier.uri http://hdl.handle.net/10394/7383
dc.description.abstract A series of fluorescent heterocyclic adamantane amines were synthesised with the goal to develop novel fluorescent ligands for neurological assay development. These derivatives demonstrated multifunctional neuroprotective activity through inhibition of the N-methyl-D-aspartate receptor/ion channel, calcium channels and the enzyme nitric oxide synthase. It also exhibited a high degree of free radical scavenging potential. N-(1-adamantyl)-2-oxo-chromene-3-carboxamide (8), N-adamantan-1-yl-5-dimethyl-amino-1-naphthalenesulfonic acid (11) and N-(1-cyano-2H-isoindol-2-yl) adamantan-1-amine (12) were found to possess a high degree of multifunctionality with favourable physical-chemical properties for bioavailability and blood-brain barrier permeability. The ability of these heterocyclic adamantane amine derivatives as nitric oxide synthase inhibitors, calcium channel modulators, NMDAR inhibitors and effective antioxidants, indicate that they may find application as multifunctional drugs in neuroprotection. en_US
dc.description.uri http://dx.doi.org/10.1016/j.bmc.2011.05.034
dc.language.iso en en_US
dc.publisher Elsevier en_US
dc.subject Amantadine en_US
dc.subject NMDA receptor en_US
dc.subject antioxidant activity en_US
dc.subject neuroprotection en_US
dc.subject calcium channels en_US
dc.subject NOS inhibition en_US
dc.title Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents en_US
dc.type Article en_US


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