title: Synthetic Medicinal Chemistry in Chagas' Disease: Compounds at The Final Stage of "Hit-To-Lead" Phase.
abstract: Chagas' disease, or American trypanosomosiasis, has been the most relevant illness produced by protozoa in Latin America. Synthetic medicinal chemistry efforts have provided an extensive number of chemodiverse hits at the "active-to-hit" stage. However, only a more limited number of these have been studiedin vivoin models of Chagas' disease. Herein, we survey some of the cantidates able to surpass the "hit-to-lead" stage discussing their limitations or merit to enter in clinical trials in the short term.
authors.affiliation: Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay. hcerecet@fq.edu.uy.
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
authors.affiliation: Laboratorio de Química Orgánica, Instituto de Química Biológica-Facultad de Ciencias, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay. megonzal@fq.edu.uy.
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
keywords: Chagas’ disease; drug-likeness; “hit-to-lead”