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Pure Appl. Chem., 2005, Vol. 77, No. 11, pp. 1957-1964

doi:10.1351/pac200577111957

Economic drug discovery and rational medicinal chemistry for tropical diseases*

Kelly Chibale

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa


Abstract: In order to fulfill research objectives around target-based drug discovery in the field of anti-infective agents that are prevalent mainly in poor Third World countries, selection of biological and chemical targets is guided by economic drug discovery and rational medicinal chemistry. Selection of biological targets of therapeutic relevance in multiple disease-causing organisms, as well as the use of natural products and existing drugs as chemical scaffolds for the discovery and design of novel therapeutics should be viable strategies underpinning drug discovery research in poor Third World countries. In this regard, biological targets of interest to our program include disulfide reductases and cysteine proteases (CPs), while chemical scaffolds include existing antimalarial agents and natural products.

Keywords: enzyme inhibitors; Malaria; medicinal chemistry; natural products; trypanosomiasis.

*Paper based on a presentation at the 9th International Chemistry Conference in Africa (ICCA-9), Arusha, Tanzania, 2-7 August 2004. Other presentations are published in this issue, pp. 1923-1964.