Chagas disease is still a worldwide threat, with estimated 6 to 7 million infected people,
mainly in Latin America. Current treatments still rely only on benznidazol and nifurtimox, drugs with
poor efficacy in chronic infection phase and recognized toxicity. Thus, there is an urgent need for new
therapeutic agents against this disease. In this review we present an updated selection over the last decade
of synthetic glycoconjugates as anti-trypanosomal agents, properly addressed as monosaccharideand
disaccharide-based agents, and multivalent-based derivatives, disclosing relevant methods for their
synthesis, along with their activities on T. cruzi and its trans-sialidase (TcTS). In addition, synthetic glycoconjugates
as potential vaccines and diagnostic antigens against T. cruzi are also reported.