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Review

Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase

by
Hugo Cerecetto
1,* and
Mercedes González
2,*
1
Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay
2
Laboratorio de Química Orgánica, Instituto de Química Biológica-Facultad de Ciencias, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2010, 3(4), 810-838; https://doi.org/10.3390/ph3040810
Submission received: 1 February 2010 / Revised: 15 March 2010 / Accepted: 19 March 2010 / Published: 25 March 2010
(This article belongs to the Special Issue Tropical Medicine)

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 studied in vivo in 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.
Keywords: Chagas’ disease; “hit-to-lead”; drug-likeness Chagas’ disease; “hit-to-lead”; drug-likeness
Graphical Abstract

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MDPI and ACS Style

Cerecetto, H.; González, M. Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase. Pharmaceuticals 2010, 3, 810-838. https://doi.org/10.3390/ph3040810

AMA Style

Cerecetto H, González M. Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase. Pharmaceuticals. 2010; 3(4):810-838. https://doi.org/10.3390/ph3040810

Chicago/Turabian Style

Cerecetto, Hugo, and Mercedes González. 2010. "Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase" Pharmaceuticals 3, no. 4: 810-838. https://doi.org/10.3390/ph3040810

APA Style

Cerecetto, H., & González, M. (2010). Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase. Pharmaceuticals, 3(4), 810-838. https://doi.org/10.3390/ph3040810

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