Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents

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dc.contributor.advisorChibale, Kellyen_ZA
dc.contributor.advisorSunassee, Suthanandaen_ZA
dc.contributor.authorShanika, Petrus Sininguen_ZA
dc.date.accessioned2018-02-12T08:57:58Z
dc.date.available2018-02-12T08:57:58Z
dc.date.issued2017en_ZA
dc.description.abstractThe causative agent of tuberculosis (TB), Mycobacterium tuberculosis (Mtb), still remains one of the most serious infectious diseases with 10 million new reported cases in 2015. Although TB is curable, the ability to acquire resistance to various antibiotics by the Mtb organism is well known. The emergence and spread of multidrug resistance (MDR) and extremely drug resistance (XDR) Mtb strains, along with HIV/TB co-infections, has put TB control programmes in jeopardy, particularly in developing countries. Therefore, there is a continuous need to search for new structural classes of anti-TB drugs with novel modes of action and ideally no cross resistance to current drugs to treat both sensitive and resistant forms of TB. Fusidic acid is a naturally occurring antibiotic used to treat Gram-positive bacterial infections. It has potent activity against S. aureus and is clinically used to treat mild to moderately severe skin and soft-tissue infections. The mode of action of fusidic acid involves the inhibition of protein synthesis via binding to bacterial elongation factor G (EF-G). Fusidic acid has also been reported to possess in vitro antimycobacterial activity but was subsequently found to lack in vivo efficacy in a mouse model. Towards contributing to new antimycobacterial agents, this study focusses on repositioning fusidic acid for tuberculosis by employing prodrug and bioisosterism approaches through structural modifications at the C-3, C-11 and C-21 positions of the drug.en_ZA
dc.identifier.apacitationShanika, P. S. (2017). <i>Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents</i>. (Thesis). University of Cape Town ,Faculty of Science ,Department of Chemistry. Retrieved from http://hdl.handle.net/11427/27536en_ZA
dc.identifier.chicagocitationShanika, Petrus Siningu. <i>"Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents."</i> Thesis., University of Cape Town ,Faculty of Science ,Department of Chemistry, 2017. http://hdl.handle.net/11427/27536en_ZA
dc.identifier.citationShanika, P. 2017. Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents. University of Cape Town.en_ZA
dc.identifier.ris TY - Thesis / Dissertation AU - Shanika, Petrus Siningu AB - The causative agent of tuberculosis (TB), Mycobacterium tuberculosis (Mtb), still remains one of the most serious infectious diseases with 10 million new reported cases in 2015. Although TB is curable, the ability to acquire resistance to various antibiotics by the Mtb organism is well known. The emergence and spread of multidrug resistance (MDR) and extremely drug resistance (XDR) Mtb strains, along with HIV/TB co-infections, has put TB control programmes in jeopardy, particularly in developing countries. Therefore, there is a continuous need to search for new structural classes of anti-TB drugs with novel modes of action and ideally no cross resistance to current drugs to treat both sensitive and resistant forms of TB. Fusidic acid is a naturally occurring antibiotic used to treat Gram-positive bacterial infections. It has potent activity against S. aureus and is clinically used to treat mild to moderately severe skin and soft-tissue infections. The mode of action of fusidic acid involves the inhibition of protein synthesis via binding to bacterial elongation factor G (EF-G). Fusidic acid has also been reported to possess in vitro antimycobacterial activity but was subsequently found to lack in vivo efficacy in a mouse model. Towards contributing to new antimycobacterial agents, this study focusses on repositioning fusidic acid for tuberculosis by employing prodrug and bioisosterism approaches through structural modifications at the C-3, C-11 and C-21 positions of the drug. DA - 2017 DB - OpenUCT DP - University of Cape Town LK - https://open.uct.ac.za PB - University of Cape Town PY - 2017 T1 - Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents TI - Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents UR - http://hdl.handle.net/11427/27536 ER - en_ZA
dc.identifier.urihttp://hdl.handle.net/11427/27536
dc.identifier.vancouvercitationShanika PS. Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents. [Thesis]. University of Cape Town ,Faculty of Science ,Department of Chemistry, 2017 [cited yyyy month dd]. Available from: http://hdl.handle.net/11427/27536en_ZA
dc.language.isoengen_ZA
dc.publisher.departmentDepartment of Chemistryen_ZA
dc.publisher.facultyFaculty of Scienceen_ZA
dc.publisher.institutionUniversity of Cape Town
dc.subject.otherChemistryen_ZA
dc.titleSemi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agentsen_ZA
dc.typeMaster Thesis
dc.type.qualificationlevelMasters
dc.type.qualificationnameMScen_ZA
uct.type.filetypeText
uct.type.filetypeImage
uct.type.publicationResearchen_ZA
uct.type.resourceThesisen_ZA
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