Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense
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 scaf...
| Main Authors: | , , , , , |
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| Format: | Journal Article |
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Wiley - V C H Verlag GmbH & Co. KGaA
2016
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| Online Access: | http://hdl.handle.net/20.500.11937/51609 |
| _version_ | 1848758739936477184 |
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| author | Cullen, Danica Pengon, J. Rattanajak, R. Chaplin, J. Kamchonwongpaisan, S. Mocerino, Mauro |
| author_facet | Cullen, Danica Pengon, J. Rattanajak, R. Chaplin, J. Kamchonwongpaisan, S. Mocerino, Mauro |
| author_sort | Cullen, Danica |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T09:48:47Z |
| format | Journal Article |
| id | curtin-20.500.11937-51609 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T09:48:47Z |
| publishDate | 2016 |
| publisher | Wiley - V C H Verlag GmbH & Co. KGaA |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-516092017-06-20T05:49:43Z Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense Cullen, Danica Pengon, J. Rattanajak, R. Chaplin, J. Kamchonwongpaisan, S. Mocerino, Mauro 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. 2016 Journal Article http://hdl.handle.net/20.500.11937/51609 Wiley - V C H Verlag GmbH & Co. KGaA restricted |
| spellingShingle | Cullen, Danica Pengon, J. Rattanajak, R. Chaplin, J. Kamchonwongpaisan, S. Mocerino, Mauro Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title | Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title_full | Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title_fullStr | Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title_full_unstemmed | Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title_short | Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense |
| title_sort | scoping studies into the structure-activity relationship (sar) of phenylephrine-derived analogues as inhibitors of trypanosoma brucei rhodesiense |
| url | http://hdl.handle.net/20.500.11937/51609 |