Chemotherapy of African Trypanosomiasis

Abstract

There is a critical need for new effective chemotherapeutic agents against the African Trypanosomes. At the present time, drug research is primarily focused on the molecular target approach, however, it is suggested that a more balanced approach involving screening against the whole organism be given greater emphasis. To illustrate this point, recent research involving the screening of new compounds derived from pentamidine is discussed. Analogues with improved chemotherapeutic potential have been obtained. Based upon the chemical structures of these lead compounds and a mode of action hypothesis the synthesis of novel trypanocidal drugs are in progress. Current data suggests that pentamidine analogues with oral bioavailability, as well as better blood-brain barrier transport have been developed. It is suggested that enlightened whole organism screening of analogues of the currently used chemotherapeutic agents will lead to the more rapid development of new trypanocidal drugs.