Issue in Honor of Prof. James Bull ARKIVOC 2002 (ix) 93-98
Towards broadspectrum antiprotozoal agents Kelly Chibale*
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa E-mail: chibale@science.uct.ac.za
Dedicated with great respect and admiration to Professor James R. Bull on the occasion of his retirement
Abstract
Since the market for antiparasitic drugs is in poor Third World countries, innovative and cost effective approaches to antiparasite drug discovery and development are urgently needed. Development of broadspectrum antiprotozoal agents acting against multiple protozoan parasites offers numerous advantages in addressing the challenges inherent in the aforementioned approaches. With a view to addressing these challenges, our research group at the University of Cape Town has initiated research projects whose main objectives include: (i) the development of single agents that provide target-directed inhibition of multiple protozoans; (ii) the development of single agents that provide maximal antiprotozoan activity by acting against multiple parasitic targets. The human diseases of leishmaniasis, malaria and trypanosomiasis have been selected for proof of concept studies with cysteine proteases and oxidoreductases present in the respective parasites selected as enzyme targets for antileishmanial, antimalarial and antitrypanosomal drug discovery efforts.
Keywords: Cysteine proteases, trypanothione reductase, trypanosomiasis, leishmaniasis, malaria
Introduction
Current chemotherapy for malaria, trypanosomiasis and leishmaniasis is inadequate, toxic or both. While potential demand for antiparasitic drugs in endemic areas is high, drug resistance to established drugs is a major problem. Previous first line drugs have been rendered completely ineffective in most endemic areas. Understanding of the mechanism of resistance and development of chemical agents without cross-resistance to existing drugs is of paramount importance. Since the market for antiparasitic drugs is in poor Third World countries, innovative and cost effective approaches to antiparasite drug discovery and development are urgently needed.
ISSN 1424-6376 Page 93 ©ARKAT USA, Inc
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