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Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis
Includes bibliographical references (leaves 131-141).
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| Main Author: | |
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| Other Authors: | |
| Format: | Thesis |
| Language: | English |
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Division of Immunology
2014
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| _version_ | 1867613646578778112 |
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| access_status_str | Open Access |
| author | Sebesho, Biopelo Felicity |
| author2 | Jacobs, Muazzam |
| author_browse | Jacobs, Muazzam Sebesho, Biopelo Felicity |
| author_facet | Jacobs, Muazzam Sebesho, Biopelo Felicity |
| author_sort | Sebesho, Biopelo Felicity |
| collection | Thesis |
| description | Includes bibliographical references (leaves 131-141). |
| format | Thesis |
| id | oai:open.uct.ac.za:11427/3116 |
| institution | University of Cape Town (South Africa) |
| language | eng |
| last_indexed | 2026-06-10T12:39:27.712Z |
| license_str | Not specified — see source repository |
| provenance_str_mv | Harvested via OAI-PMH from UCTD — University of Cape Town Open Access Repository |
| publishDate | 2014 |
| publishDateRange | 2014 |
| publishDateSort | 2014 |
| publisher | Division of Immunology |
| publisherStr | Division of Immunology |
| record_format | dspace |
| source_str | UCTD — University of Cape Town Open Access Repository |
| spelling | oai:open.uct.ac.za:11427/3116 Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis Sebesho, Biopelo Felicity Jacobs, Muazzam Medicine Includes bibliographical references (leaves 131-141). Tuberculosis remains an important public health problem worldwide. There has been increase in the development of drug resistance towards INH and RIF, two of the frontline antimycobacterial drugs currently used in therapeutic regimes. As an attempt to address drug resistance, the World Health Organization has implemented the DOTS strategy in 182 countries. Moreover, new chemical libraries of potential antituberculosis drugs have been designed and synthesised. We therefore assessed 121 derivatives from the acetolactate synthase inhibitors, cysteine protease inhibitors, thiosemicarbazones, and thiolactomycins classes of compounds for in vitro efficacy against M. tuberculosis using the resazurin microtitre plate assay afterwhich active compounds were assessed for cytotoxicity in vitro against elicited peritoneal macrophages using the MTT assay. Of the 38 acetolactate synthase inhibitors tested, 2 derivatives namely RKG162A and RKG1541 were bactericidal against M. tuberculosis. Both derivatives were mildly cytotoxic against macrophages. For cysteine protease inhibitors, 35 derivatives were tested. Four derivatives namely AXE1, AXE4, AXE5, and AXE29 were bactericidal whereas AXE2, AXE3, AXE35, and NAT47 were bacteriostatic. 2014-07-28T14:54:08Z 2014-07-28T14:54:08Z 2006 Master Thesis Masters MSc http://hdl.handle.net/11427/3116 eng application/pdf Division of Immunology Faculty of Health Sciences University of Cape Town |
| spellingShingle | Medicine Sebesho, Biopelo Felicity Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| thesis_degree_str | Master's |
| title | Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| title_full | Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| title_fullStr | Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| title_full_unstemmed | Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| title_short | Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis |
| title_sort | investigation of the efficacy of identified acetolactate synthase inhibitors peptidyl cysteine protease inhibitors thiolactomycins and thiosemicarbazone compounds against mycobacterium tuberculosis |
| topic | Medicine |
| url | http://hdl.handle.net/11427/3116 |
| work_keys_str_mv | AT sebeshobiopelofelicity investigationoftheefficacyofidentifiedacetolactatesynthaseinhibitorspeptidylcysteineproteaseinhibitorsthiolactomycinsandthiosemicarbazonecompoundsagainstmycobacteriumtuberculosis |