A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria

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dc.contributor.advisorChibale, Kellyen_ZA
dc.contributor.authorKaur, Gurminderen_ZA
dc.date.accessioned2017-01-26T13:59:22Z
dc.date.available2017-01-26T13:59:22Z
dc.date.issued2016en_ZA
dc.description.abstractTuberculosis (TB) and malaria continue to be major public health concerns, globally claiming 2-3 million deaths every year. A number of efficacious drugs are available for the treatment of TB and malaria, which, through various combination therapies, are fully effective in treating these diseases. However, the wide spread resistance in M. tuberculosis (Mtb) and P. falciparum, the causative agents of TB and malaria, respectively, has made the existing therapies less effective. Thus novel agents able to circumvent drug resistance and other challenges associated with existing TB and malaria treatments are urgently needed. The development of a new drug is a lengthy and costly process; therefore, approaches that can save both time and money need to be emphasised. Drug repositioning is one such approach that has been applied in this project. Drug repositioning basically involves a situation where a drug active in one disease is derivatised or used as a template for the synthesis of derivatives active in another disease. This approach has the potential to significantly shorten the drug discovery process. This study focused on the repositioning of two drugs, the antibacterial agent fusidic acid and the antipsychotic agent metergoline, in TB and/or malaria via medicinal chemistry approaches. New semisynthetic derivatives of fusidic acid and metergoline were synthesized and evaluated for antimycobacterial activity against the H37Rv strain of Mtb and antiplasmodial activity against the NF54 strain of P. falciparum.en_ZA
dc.identifier.apacitationKaur, G. (2016). <i>A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria</i>. (Thesis). University of Cape Town ,Faculty of Science ,Department of Chemistry. Retrieved from http://hdl.handle.net/11427/23462en_ZA
dc.identifier.chicagocitationKaur, Gurminder. <i>"A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria."</i> Thesis., University of Cape Town ,Faculty of Science ,Department of Chemistry, 2016. http://hdl.handle.net/11427/23462en_ZA
dc.identifier.citationKaur, G. 2016. A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria. University of Cape Town.en_ZA
dc.identifier.ris TY - Thesis / Dissertation AU - Kaur, Gurminder AB - Tuberculosis (TB) and malaria continue to be major public health concerns, globally claiming 2-3 million deaths every year. A number of efficacious drugs are available for the treatment of TB and malaria, which, through various combination therapies, are fully effective in treating these diseases. However, the wide spread resistance in M. tuberculosis (Mtb) and P. falciparum, the causative agents of TB and malaria, respectively, has made the existing therapies less effective. Thus novel agents able to circumvent drug resistance and other challenges associated with existing TB and malaria treatments are urgently needed. The development of a new drug is a lengthy and costly process; therefore, approaches that can save both time and money need to be emphasised. Drug repositioning is one such approach that has been applied in this project. Drug repositioning basically involves a situation where a drug active in one disease is derivatised or used as a template for the synthesis of derivatives active in another disease. This approach has the potential to significantly shorten the drug discovery process. This study focused on the repositioning of two drugs, the antibacterial agent fusidic acid and the antipsychotic agent metergoline, in TB and/or malaria via medicinal chemistry approaches. New semisynthetic derivatives of fusidic acid and metergoline were synthesized and evaluated for antimycobacterial activity against the H37Rv strain of Mtb and antiplasmodial activity against the NF54 strain of P. falciparum. DA - 2016 DB - OpenUCT DP - University of Cape Town LK - https://open.uct.ac.za PB - University of Cape Town PY - 2016 T1 - A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria TI - A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria UR - http://hdl.handle.net/11427/23462 ER - en_ZA
dc.identifier.urihttp://hdl.handle.net/11427/23462
dc.identifier.vancouvercitationKaur G. A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria. [Thesis]. University of Cape Town ,Faculty of Science ,Department of Chemistry, 2016 [cited yyyy month dd]. Available from: http://hdl.handle.net/11427/23462en_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.titleA medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malariaen_ZA
dc.typeDoctoral Thesis
dc.type.qualificationlevelDoctoral
dc.type.qualificationnamePhDen_ZA
uct.type.filetypeText
uct.type.filetypeImage
uct.type.publicationResearchen_ZA
uct.type.resourceThesisen_ZA
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