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Abstract:

We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at low micromolar level. Cellular activity was associated with the inhibition of enzymatic activity of T. cruzi farnesyl pyrophosphate synthase. As bisphosphonate-containing drugs are FDA-approved for the treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. © 2005 Elsevier Ltd. All rights reserved.

Registro:

Documento: Artículo
Título:Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
Autor:Szajnman, S.H.; Ravaschino, E.L.; Docampo, R.; Rodriguez, J.B.
Filiación:Departamento de Química Orgánica, Facultad de Ciencias Exactas Y Naturales, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina
Center for Global and Emerging Diseases, Department of Cellular Biology, University of Georgia, Athens, GA 30602, United States
Palabras clave:Bisphosphonates; Chagas' disease; Farnesyl pyrophosphate synthase; Trypanosoma cruzi; bisphosphonic acid derivative; fatty acid; geranyltransferase; protozoal protein; antiprotozoal activity; article; cell proliferation; Chagas disease; drug synthesis; drug targeting; enzyme inhibition; IC 50; nonhuman; Trypanosoma cruzi; Animals; Antiprotozoal Agents; Diphosphonates; Drug Delivery Systems; Fatty Acids; Inhibitory Concentration 50; Pyrophosphatases; Structure-Activity Relationship; Trypanosoma cruzi; Trypanosoma cruzi
Año:2005
Volumen:15
Número:21
Página de inicio:4685
Página de fin:4690
DOI: http://dx.doi.org/10.1016/j.bmcl.2005.07.060
Título revista:Bioorganic and Medicinal Chemistry Letters
Título revista abreviado:Bioorg. Med. Chem. Lett.
ISSN:0960894X
CODEN:BMCLE
CAS:geranyltransferase, 37277-79-5, 50812-36-7; Antiprotozoal Agents; Diphosphonates; farnesyl pyrophosphatase, EC 3.6.1.-; Fatty Acids; Pyrophosphatases, EC 3.6.1.-
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v15_n21_p4685_Szajnman

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Citas:

---------- APA ----------
Szajnman, S.H., Ravaschino, E.L., Docampo, R. & Rodriguez, J.B. (2005) . Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase. Bioorganic and Medicinal Chemistry Letters, 15(21), 4685-4690.
http://dx.doi.org/10.1016/j.bmcl.2005.07.060
---------- CHICAGO ----------
Szajnman, S.H., Ravaschino, E.L., Docampo, R., Rodriguez, J.B. "Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase" . Bioorganic and Medicinal Chemistry Letters 15, no. 21 (2005) : 4685-4690.
http://dx.doi.org/10.1016/j.bmcl.2005.07.060
---------- MLA ----------
Szajnman, S.H., Ravaschino, E.L., Docampo, R., Rodriguez, J.B. "Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase" . Bioorganic and Medicinal Chemistry Letters, vol. 15, no. 21, 2005, pp. 4685-4690.
http://dx.doi.org/10.1016/j.bmcl.2005.07.060
---------- VANCOUVER ----------
Szajnman, S.H., Ravaschino, E.L., Docampo, R., Rodriguez, J.B. Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase. Bioorg. Med. Chem. Lett. 2005;15(21):4685-4690.
http://dx.doi.org/10.1016/j.bmcl.2005.07.060