Chagas disease is a neglected tropical disease that is endemic to Latin and Central America. Twenty-five million people are living at risk of infection in these locations, and population migration is spreading the disease to previously unaffected regions. Current therapeutics show increasing cases of treatment failure, have low efficacy, and severe side effects. However, NTDs typically suffer from a “translation innovation gap” where drugs fail to progress from in vitro drug screening to preclinical studies. We have established an integrated research network that combines academic drug discovery (Northeastern University), industry (Charles River Labs and AstraZeneca), and public-private partnerships (Drugs for Neglected Diseases <i>initiative</i>) to address the desperate need for new therapeutics for Chagas disease.<br/><br/>Recently, an innovative virtual screening campaign of five proprietary pharmaceutical company compound libraries was reported, exploring an imidazo[1,2-a]pyridine hit. We will describe our efforts to optimize this series for targeted properties for this series based upon the Target Product Profile for Chagas disease. In particular, strategies that have been used to modulate metabolism and aqueous solubility for this series will be reported.

Distributed drug discovery applied to Chagas disease

ACS Spring Meeting 2021

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