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dc.contributor.authorJoubert, Jacques
dc.contributor.authorMalan, Sarel Francois
dc.contributor.authorVan Dyk, Sandra
dc.contributor.authorGreen, Ivan R.
dc.identifier.citationJoubert, J. et al. 2011. Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents. Bioorganic & medicinal chemistry, 19(13):3935-3944. []en_US
dc.identifier.issn1464-3391 (Online)
dc.description.abstractA 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.subjectNMDA receptoren_US
dc.subjectantioxidant activityen_US
dc.subjectcalcium channelsen_US
dc.subjectNOS inhibitionen_US
dc.titleSynthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agentsen_US

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