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dc.contributor.authorCullen, Danica
dc.contributor.authorPengon, J.
dc.contributor.authorRattanajak, R.
dc.contributor.authorChaplin, J.
dc.contributor.authorKamchonwongpaisan, S.
dc.contributor.authorMocerino, Mauro
dc.date.accessioned2017-03-24T11:54:12Z
dc.date.available2017-03-24T11:54:12Z
dc.date.created2017-03-23T06:59:50Z
dc.date.issued2016
dc.identifier.citationCullen, D. and Pengon, J. and Rattanajak, R. and Chaplin, J. and Kamchonwongpaisan, S. and Mocerino, M. 2016. Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense. ChemistrySelect. 1 (15): pp. 4533-4538.
dc.identifier.urihttp://hdl.handle.net/20.500.11937/51609
dc.description.abstract

Human African Trypanosomiasis (HAT) is a disease caused by the parasite Trypanosoma brucei and is classified as a neglected tropical disease of concern in sub-Saharan Africa. A scoping study has been undertaken to develop a preliminary structure activity relationship of a tetrahydroisoquinoline scaffold. Fourteen compounds based around this core scaffold were synthesised and evaluated for their activity against Trypanosoma brucei rhodesiense in vitro. Initial results are promising with a number of analogues showing low micromolar inhibition of T.b.rhodesiense with acceptable selectivity over mammalian cells. The most promising is a secondary amine analogue showing the most potent inhibition of T.b.rhodesiense, with an IC50 value of 0.25 ± 0.02 µM, while also showing low cytotoxicity to mammalian cells.

dc.publisherWiley - V C H Verlag GmbH & Co. KGaA
dc.titleScoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense
dc.typeJournal Article
dcterms.source.volume1
dcterms.source.startPage4533
dcterms.source.endPage4538
dcterms.source.issn2365-6549
dcterms.source.titleChemistrySelect
curtin.departmentDepartment of Chemistry
curtin.accessStatusFulltext not available


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