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Abstract:

Studies on the mode of action of a series of bisphosphonates derived from fatty acids, which had previously proved to be potent inhibitors against Trypanosoma cruzi proliferation in in vitro assays, have been performed. Some of these drugs proved to be potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at the low micromolar level. As bisphosphonates are FDA clinically approved for treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. © 2003 Elsevier Ltd. All rights reserved.

Registro:

Documento: Artículo
Título:Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase
Autor:Szajnman, S.H.; Montalvetti, A.; Wang, Y.; Docampo, R.; Rodriguez, J.B.
Filiación:Depto. de Quím. Orgán., Fac. de Ciencias Exactas y Naturales, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina
Department of Pathobiology, Center for Zoonoses Research, Univ. of IL at Urbana-Champaign, 2001 South Lincoln Avenue, Urbana, IL 61802, United States
Palabras clave:fatty acid derivative; geranyltransferase; phosphonic acid derivative; anorexia; article; cell proliferation; drug approval; drug potency; food and drug administration; IC 50; in vitro study; inhibition kinetics; nonhuman; osteolysis; parasite; peripheral neuropathy; skin allergy; tropical disease; Trypanosoma cruzi; vomiting; Trypanosoma; Trypanosoma cruzi
Año:2003
Volumen:13
Número:19
Página de inicio:3231
Página de fin:3235
DOI: http://dx.doi.org/10.1016/S0960-894X(03)00663-2
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
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v13_n19_p3231_Szajnman

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Citas:

---------- APA ----------
Szajnman, S.H., Montalvetti, A., Wang, Y., Docampo, R. & Rodriguez, J.B. (2003) . Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase. Bioorganic and Medicinal Chemistry Letters, 13(19), 3231-3235.
http://dx.doi.org/10.1016/S0960-894X(03)00663-2
---------- CHICAGO ----------
Szajnman, S.H., Montalvetti, A., Wang, Y., Docampo, R., Rodriguez, J.B. "Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase" . Bioorganic and Medicinal Chemistry Letters 13, no. 19 (2003) : 3231-3235.
http://dx.doi.org/10.1016/S0960-894X(03)00663-2
---------- MLA ----------
Szajnman, S.H., Montalvetti, A., Wang, Y., Docampo, R., Rodriguez, J.B. "Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase" . Bioorganic and Medicinal Chemistry Letters, vol. 13, no. 19, 2003, pp. 3231-3235.
http://dx.doi.org/10.1016/S0960-894X(03)00663-2
---------- VANCOUVER ----------
Szajnman, S.H., Montalvetti, A., Wang, Y., Docampo, R., Rodriguez, J.B. Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase. Bioorg. Med. Chem. Lett. 2003;13(19):3231-3235.
http://dx.doi.org/10.1016/S0960-894X(03)00663-2