This work addresses the synthesis and biological evaluation of glycosyl diketopiperazines (DKPs) cyclo [Asp-(αGalNAc) Ser] 3 and cyclo [Asp-(αGalNAc) Thr] 4 for the development of novel anti-trypanosomal agents and Trypanosoma cruzi trans-sialidase (TcTS) inhibitors. The target compounds were synthetized by coupling reactions between glycosyl amino acids αGalNAc-Ser 7 or αGalNAc-Thr 8 and the amino acid (O-tBu)-Asp 17, followed by ...