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

doi:10.3390/ph3040810

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Pharmaceuticals 2010, 3(4), 810-838; doi:10.3390/ph3040810

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

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.

Received: 1 February 2010; in revised form: 15 March 2010 / Accepted: 19 March 2010 / Published: 25 March 2010

(This article belongs to the Special Issue Tropical Medicine)

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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

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Cite This Article

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.

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.

Chicago/Turabian Style

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

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