Antimalarial and cysteine protease inhibitor pharmacophores as scaffolds for new antimalarial agents
Doctoral Thesis
2005
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University of Cape Town
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Abstract
The work in this thesis is threefold: (i) A new series of antiplasmodial agents were initially designed based on the β-amino alcohol bioactiphore, a subunit that is found in a number of antimalarial agents. (ii) Various thiosemicarbozones and semicarbozones were designed and synthesized as potential mechanism-based inhibiotrs of parasitic cysteine proteases. (iii) Multicomponenet reactions offer the advantage of introducing chemical diversity in fewer steps than conventional multi step organic synthesis. New chloroquine-type compounds were designed and synthesized using the Ugi 4 component condensation reaction and its variants. The synthesized compounds ranged from simple peptidic molecules to rigid heterocycles.
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Includes bibliographical references.
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Musonda, C. 2005. Antimalarial and cysteine protease inhibitor pharmacophores as scaffolds for new antimalarial agents. University of Cape Town.