Synthesis and Antichagastic Evaluation of Novel Drug Scaffolds (360G-Wellcome-211700_Z_18_Z)

Neglected Tropical Diseases (NTDs) affect more than one billion people per year and have a severe impact on the economy of developing countries. This threat is heightened for communities affected by poverty, poor sanitary infrastructure and contact with transmission vectors or infected livestock. Chagas disease, part of the NTDs is a potentially life-threatening disease caused by Trypanosoma cruzi parasites, and is commonly spread by infected triatomine bugs. Up to 10 million people are estimated to be infected worldwide, predominantly in endemic countries such as Latin America but the disease is spreading to non-disease endemic locations such as Europe, the United States of America and Canada. Benznidazole and Nifurtimox are the only approved medicines for use by the World Health Organisation but these drugs are ineffective in treating the chronic phase of the disease and have potentially fatal side-effects. Dr Bhambra’s research group has identified a novel drug scaffold displaying antichagastic activities whist remaining non-toxic to mammalian cells. Therefore, this scholarship will include the design, syntheses and safety screening of further novel compounds with drug-like properties, and aim to deliver molecules with greater on-target potency and reduced off-target effects leading to promising compounds suitable for further preclinical investigation.