Search of new chemotherapeutic agents against parasitic diseases.

GUILLERMO LABADIE; ESTEBAN PANOZZO; EXEQUIEL PORTA; SHANE WILKINSON; BABU TEKWANI

Copper Mountain, CO, USA

Simposio; Molecular Targets for Control of Vector-Borne Diseases: Bridging Lab and Field Research (F2); 2010

Keystone Symposia on molecular and cellular biology

In our search of new chemotherapies against vector borne parasitic diseases we have focused on different essential biosynthetic pathways as target to developed new chemotherapeutic agents. Over 300 new compounds were prepared using conventional synthetic procedures. Libraries were tested against the parasites responsible of the visceral leishmaniasis (L. donovani) malaria (P. falciparum, Chloroquine sensitive and resistant strains) Human African tripanosomiasis (T. brucei) and Chagas’ disease (T. cruzi). As result of our effort we have found promising compounds for all the parasites tested with submicromolar to nanomolar IC50s. Based on the structure of the scaffold used on each library prepared interesting structure-activity profile of were found. Experiments to validate the metabolic pathway targeted and the future optimization of heat compounds found will be discuss. Acknowledgments: This investigation received financial support from the UNICEF/UNDP/WORLD BANK/WHO Special Programme for Research and Training in Tropical Diseases (TDR).