Utilization of the Baylis-Hillman and related reactions in antiparasitic drug discovery

• Main Author: Mabizela, Nontobeko
• Other Authors: Chibale, Kelly
• Format: Dissertation
• Language: English
• Published: University of Cape Town 2014
• Subjects: Chemistry
• Online Access: http://hdl.handle.net/11427/6325

Bibliography: leaves 81-83. === Baylis-Hillman adducts and compounds containing quinoline moieties have been previously utilized extensively in the search for antiparasitic agents. Work in this dissertation describes a series of compounds based on the Baylis-Hillman and the related three-component aza Baylis-Hillman reactions synthesised for biological evaluation as potential inhibitors of two parasitic cysteine proteases (cruzain and Falcipain-2) and as antiparasitic agents. The utilization of polymer-supported bases in the Baylis-Hillman reaction is described. The use of ultrasound in combination with Lewis acids is also described in an attempt to improve the reaction rate.