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Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis

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dc.contributor.author Van der Westhuyzen, Christiaan W
dc.contributor.author Haynes, J
dc.contributor.author Panayides, Jenny-Lee
dc.contributor.author Wiid, I
dc.contributor.author Parkinson, C
dc.date.accessioned 2021-03-29T10:01:56Z
dc.date.available 2021-03-29T10:01:56Z
dc.date.issued 2020
dc.identifier.citation Van der Westhuyzen, C.W., Haynes, J., Panayides, J., Wiid, I. & Parkinson, C. 2020. Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis. <i>Medicinal Chemistry, 16(3).</i> http://hdl.handle.net/10204/11927 en_ZA
dc.identifier.issn 1573-4064
dc.identifier.issn 1875-6638
dc.identifier.uri http://hdl.handle.net/10204/11927
dc.description.abstract Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H37Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro. Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents. Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis. en_US
dc.format Abstract en_US
dc.language.iso en en_US
dc.relation.uri https://doi.org/10.2174/1573406415666190430143535 en_US
dc.relation.uri DOI: 10.2174/1573406415666190430143535 en_US
dc.relation.uri https://www.eurekaselect.com/171922/article en_US
dc.relation.uri https://pubmed.ncbi.nlm.nih.gov/31208310/ en_US
dc.source Medicinal Chemistry, 16(3) en_US
dc.subject Antitubercular activity en_US
dc.subject Artemisinin en_US
dc.subject Mycobacterium tuberculosis en_US
dc.subject Peroxide en_US
dc.subject Pyrimidine en_US
dc.subject Tetraoxane en_US
dc.title Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis en_US
dc.type Article en_US
dc.description.pages 392-402 en_US
dc.description.note Copyright: 2020 Bentham Science Publishers Ltd. This is the abstract version of the work. For access to the fulltext, kindly visit the publisher's website. en_US
dc.description.cluster Chemicals en_US
dc.description.impactarea Pharmaceutical Technologies en_US
dc.identifier.apacitation Van der Westhuyzen, C. W., Haynes, J., Panayides, J., Wiid, I., & Parkinson, C. (2020). Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis. <i>Medicinal Chemistry, 16(3)</i>, http://hdl.handle.net/10204/11927 en_ZA
dc.identifier.chicagocitation Van der Westhuyzen, Christiaan W, J Haynes, Jenny-Lee Panayides, I Wiid, and C Parkinson "Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis." <i>Medicinal Chemistry, 16(3)</i> (2020) http://hdl.handle.net/10204/11927 en_ZA
dc.identifier.vancouvercitation Van der Westhuyzen CW, Haynes J, Panayides J, Wiid I, Parkinson C. Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis. Medicinal Chemistry, 16(3). 2020; http://hdl.handle.net/10204/11927. en_ZA
dc.identifier.ris TY - Article AU - Van der Westhuyzen, Christiaan W AU - Haynes, J AU - Panayides, Jenny-Lee AU - Wiid, I AU - Parkinson, C AB - Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H37Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro. Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents. Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis. DA - 2020 DB - ResearchSpace DP - CSIR J1 - Medicinal Chemistry, 16(3) KW - Antitubercular activity KW - Artemisinin KW - Mycobacterium tuberculosis KW - Peroxide KW - Pyrimidine KW - Tetraoxane LK - https://researchspace.csir.co.za PY - 2020 SM - 1573-4064 SM - 1875-6638 T1 - Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis TI - Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis UR - http://hdl.handle.net/10204/11927 ER - en_ZA
dc.identifier.worklist 24360 en_US


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