- Title
- Exploring Quinolinyl-Thiazolidinedione hybrid compounds as potential anti-tubercular agents
- Creator
- Mtshare, Thanduxolo Elihle
- Subject
- Quinoline
- Subject
- Mycobacterium tuberculosis
- Subject
- Tuberculosis -- Chemotherapy
- Subject
- Plasmodium falciparum
- Subject
- Thiazolidinedione
- Date Issued
- 2020
- Date
- 2020
- Type
- Thesis
- Type
- Masters
- Type
- MSc
- Identifier
- http://hdl.handle.net/10962/143314
- Identifier
- vital:38232
- Description
- Tuberculosis (TB) is an infectious disease caused by the pathogen, Mycobacterium tuberculosis. According to the World Health Organization, TB is the ninth leading cause of death worldwide ranking above HIV/AIDS. This high mortality rate of TB begs the questions about the efficiency of the current therapy and raises an urgent need to create novel anti-tuberculosis agents which will aid in curbing this burden. Quinoline containing compounds have remarkable biological activities across a wide spectrum of diseases including anti-tuberculosis. On the other hand, thiazolidinedione containing compounds possess a broad spectrum of biological properties. In this study, we rationally designed compounds containing these pharmacophoric units and investigated them for their potential biological activity against Mycobacterium tuberculosis. Considering antimalarial activity of quinoline-based compounds, the compounds achieved were also cross-screened for their activity against the Plasmodium falciparum parasite, a causative agent of malaria. In all the synthesized compounds, compound 2.6a, 2.6b and 2.7b emerged as most active compounds against the H37Rv strain with MIC₉₀ values ranging in between of 1.08 – 17.1 μM. In addition, none of the compounds showed any inhibitory activities against the 3D7 strain of P. falciparum parasite. All the compounds prepared in this study showed no significant human cytotoxic effects as measured by HeLa cell line.
- Format
- 98 pages
- Format
- Publisher
- Rhodes University
- Publisher
- Faculty of Science, Chemistry
- Language
- English
- Rights
- Mtshare, Thanduxolo Elihle
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| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | MTSHARE-MSC-TR20-212.pdf | 2 MB | Adobe Acrobat PDF | View Details Download |