- Title
- Synthesis, in vitro cytotoxicity and trypanocidal evaluation of novel 1, 3, 6-substituted non-fluoroquinolones
- Creator
- Beteck, Richard M, Isaacs, Michelle, Khanye, Setshaba D, Hoppe, Heinrich C
- Date
- 2018
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/123140
- Identifier
- vital:35409
- Identifier
- https://doi.org/10.17159/0379-4350/2018/v71a25
- Description
- Sleeping sickness (trypanosomiasis) is a neglected tropical disease that affects mostly the poorest communities in sub-Saharan Africa. Toxic side effects associated with the use of current anti-trypanosomal drugs, which in some cases kill faster than the disease itself, necessitate the search for new drugs with better safety margins. To this effect, a small library bearing different substituents at position -1, -3, and -6 of the quinolone nucleus were synthesized and evaluated in vitro against HeLa cell lines and Trypanosoma brucei brucei for cytotoxicity and trypanocidal potentials, respectively. While most of these compounds showed no cytotoxic effect, they exhibited moderate to weak anti-trypanosomal activities. The SAR studies of this series provide new information worth considering in future exploration of the quinolone scaffold in search ofmore potent and safe trypanocidal agents.
- Format
- 39 pages, pdf
- Language
- English
- Relation
- South African Journal of Chemistry, Beteck, R.M., Isaacs, M., Hoppe, H.C. and Khanye, S.D., 2018. Synthesis, in vitro cytotoxicity and trypanocidal evaluation of novel 1, 3, 6-substituted non-fluoroquinolones. South African Journal of Chemistry, 71(1), pp.188-195., South African Journal of Chemistry number 71 188 195 2018 1996-840X
- Rights
- South African Journal of Chemistry
- Rights
- Use of this resource is governed by the terms and conditions of the South African Journal of Chemistry Open Access Statement (http://www.scielo.org.za/revistas/sajc/iaboutj.htm)
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Isaacs, Michelle (Mrs)
RU Centre for Chemico- and Biomedicinal Research (CCBR)
Hoppe, Heinrich C (Prof)
RU Department of Pharmacy
Khanye, David Setshaba (Associate Prof)
RU Department of Biochemistry, Microbiology and Biotechnology
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | 25.pdf | 4 MB | Adobe Acrobat PDF | View Details Download |