Neglected tropical diseases, such as Chagas disease caused by Trypanosoma cruzi, remain a critical global health problem, particularly in underprivileged communities. Our research aims to develop potential therapeutic agents by synthesizing and characterizing analogues of aureothin, a polyketide with known antiparasitic activity.
In line with the principles of green chemistry, our approach integrates computational chemistry to screen for molecules with favorable pharmacokinetic properties, significantly reducing the need for extensive experimental synthesis and minimizing resource consumption. We have successfully synthesized 12 1,2,3-triazole analogs and 11 amine analogs with yields exceeding 66% and 77%, respectively. The use of high-yield synthetic routes reduces waste generation and improves the sustainability of the process.
Future work will focus on further optimizing the synthetic methods to incorporate greener solvents, while also exploring alternative energy-efficient reaction conditions. These efforts are consistent with the principles of waste minimization, atom economy, and the use of safer reaction conditions.