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Molecules 2017, 22(1), 82; doi:10.3390/molecules22010082

Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites

1
Departamento de Química Orgánica and UMYMFOR (CONICET–FCEyN), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina
2
Center for Tropical and Emerging Global Diseases and Department of Cellular Biology, University of Georgia, Athens, GA 30602, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Artur Silva
Received: 31 October 2016 / Revised: 28 December 2016 / Accepted: 30 December 2016 / Published: 4 January 2017
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Abstract

Based on crystallographic data of the complexes 2-alkyl(amino)ethyl-1,1-bisphosphonates–Trypanosoma cruzi farnesyl diphosphate synthase, some linear 1,1-bisphosphonic acids and other closely related derivatives were designed, synthesized and biologically evaluated against T. cruzi, the responsible agent of Chagas disease and against Toxoplasma gondii, the etiologic agent of toxoplasmosis and also towards the target enzymes farnesyl pyrophosphate synthase of T. cruzi (TcFPPS) and T gondii (TgFPPS), respectively. The isoprenoid-containing 1,1-bisphosphonates exhibited modest antiparasitic activity, whereas the linear α-fluoro-2-alkyl(amino)ethyl-1,1-bisphosphonates were unexpectedly devoid of antiparasitic activity. In spite of not presenting efficient antiparasitic activity, these data turned out to be very important to establish a structural activity relationship. View Full-Text
Keywords: bisphosphonates; farnesyl diphosphate synthase; Trypanosoma cruzi; Toxoplasma gondii; Chagas disease; toxoplasmosis; antiparasitic agents bisphosphonates; farnesyl diphosphate synthase; Trypanosoma cruzi; Toxoplasma gondii; Chagas disease; toxoplasmosis; antiparasitic agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Galaka, T.; Ferrer Casal, M.; Storey, M.; Li, C.; Chao, M.N.; Szajnman, S.H.; Docampo, R.; Moreno, S.N.J.; Rodriguez, J.B. Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites. Molecules 2017, 22, 82.

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