van Ree, T.Ramaite, I. D. I.Nethavhani, Sedzani A.2017-08-102017-08-102015-05Nethavhani, Sedzani A. 2015. Design and synthesis of potential malaria cysteinyl protease inhibitors. . . http://hdl.handle.net/11602/796http://hdl.handle.net/11602/796MSc (Chemistry)Department of ChemistryThe overall objective of this project was to design and synthesize cysteinyl protease inhibitors that are envisaged to have antimalarial activity. Several synthesis routes leading to the rigid heterocyclic 2-pyridone scaffold were explored. The syntheses of the 2-pyridones involved constructing and investigating derivatives with hydrophilic and hydrophobic moieties, using a methodology that seems to have a wide scope. Intermediates as well as the target pyridones were docked into the falcipain-2 active site and tested against chloroquine­ sensitive and resistant Plasmodium falciparum strains; three 3-cyano-2-pyridones showed promising results. Using this collection of synthesis methodologies, a wide variety of di- and tripeptides based on a substituted 2-pyridone scaffold in the P2 position, have become accessible.1 online resource (viii, 93 leaves): color illustrations)enUniversity of VendaPlasmodium proteaseUCTDCysteinase2-pyridoneAntimalarial614.532MalariaMalaria -- PreventionMalaria -- ChemotherapyPlasmodiumDissertationNethavhani Sedzani A. Design and synthesis of potential malaria cysteinyl protease inhibitors. []. , 2015 [cited yyyy month dd]. Available from: http://hdl.handle.net/11602/796Nethavhani, Sedzani A. (2015). <i>Design and synthesis of potential malaria cysteinyl protease inhibitors</i>. (). . Retrieved from http://hdl.handle.net/11602/796Nethavhani, Sedzani A.. <i>"Design and synthesis of potential malaria cysteinyl protease inhibitors."</i> ., , 2015. http://hdl.handle.net/11602/796TY - Dissertation AU - Nethavhani, Sedzani A. AB - See the attached abstract below DA - 2015-05 DB - ResearchSpace DP - Univen KW - Plasmodium protease KW - Cysteinase KW - 2-pyridone KW - Antimalarial LK - https://univendspace.univen.ac.za PY - 2015 T1 - Design and synthesis of potential malaria cysteinyl protease inhibitors TI - Design and synthesis of potential malaria cysteinyl protease inhibitors UR - http://hdl.handle.net/11602/796 ER -