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dc.contributor.authorStrydom, B.
dc.contributor.authorBergh, J.J.
dc.contributor.authorPetzer, J.P.
dc.identifier.citationStrydom, B. et al. 2012. The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy) caffeine analogues. Arzneimittel-Forschung/Drug research, 62(11):513-518. []en_US
dc.identifier.issn1616-7066 (Online)
dc.description.abstractPrevious studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an IC50 value of 0.383 µM towards MAO-B. In an attempt to improve on the inhibition potency of this compound and to discover highly potent reversible MAO-B inhibitors, in the present study, a series of 8-(2-phenoxyethoxy)caffeine analogues containing various substituents on C4 of the phenoxy ring, were synthesized and evaluated as inhibitors of human MAO-A and -B. The results show that the 8-(2-phenoxyethoxy)caffeine analogues are selective and reversible MAO-B inhibitors with the most potent homologue, 8-{2-[4-(trifluoromethyl)phenoxy]ethoxy}caffeine, exhibiting an IC50 value of 0.061 μM. These highly potent inhibitors are useful leads in the design of therapies for neurodegenerative disorders such as Parkinson's disease.en_US
dc.subjectMonoamine oxidaseen_US
dc.subjectReversible inhibitionen_US
dc.subjectSelective inhibitionen_US
dc.subjectStructure-activity relationshipen_US
dc.titleThe inhibition of monoamine oxidase by 8-(2-phenoxyethoxy) caffeine analoguesen_US
dc.contributor.researchID10057072 - Bergh, Jacobus Johannes
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12989169 - Strydom, Belinda

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