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Abstract:

As a continuation of our project aimed at the search for new chemotherapeutic agents against Chagas' disease, several drugs structurally related to the insect growth regulator Fenoxycarb and the naturally occurring juvenfie hormone of insects were designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible of this disease. Isoprenoid derivatives (compounds 33, 34, 36, and 37) were potent growth inhibitors of Trypanosoma cruzi epimastigotes. In addition, taking into account the high activity observed for compound 30 and the inhibitory action of related compounds, the allyl ether moiety bonded at the polar extreme of these inhibitors proved to be a promising group for the design of new drugs.

Registro:

Documento: Artículo
Título:Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
Autor:Schvartzapel, A.J.; Zhong, L.; Docampo, R.; Rodriguez, J.B.; Gros, E.G.
Filiación:Depto. de Quim. Orgánica, Fac. de Ciencias Exactas y Naturales, Ciudad Universitaria, 1428 Buenos Aires, Argentina
Laboratory of Molecular Parasitology, Department of Pathobiology, Univ. Illinois at Urbana-Champaign, 2001 South Lincoln Avenue, Urbana, IL 61801, United States
Palabras clave:3,7 dimethylocta 2,6 dien 1 yl ethylcarbamate; 3,7 dimethylocta 2,6 dien 1 yl tetrahydro 2h pyran 2 yl ether; 3,7,11 trimethyldodeca 2,6,10 trien 1 yl ethylcarbamate; 3,7,11 trimethyldodeca 2,6,10 trien 1 yl tetrahydro 2h pyran 2 yl ether; 4 benzoylphenyl prop 2 en 1 yl ether; benznidazole; fenoxycarb; isoprenoid; nifurtimox; unclassified drug; article; chagas disease; drug design; drug synthesis; epimastigote; structure activity relation; trypanosoma cruzi; Animals; Drug Design; Magnetic Resonance Spectroscopy; Mass Spectrometry; Molecular Structure; Spectrophotometry, Infrared; Trypanocidal Agents; Trypanosoma cruzi
Año:1997
Volumen:40
Número:15
Página de inicio:2314
Página de fin:2322
DOI: http://dx.doi.org/10.1021/jm9607616
Título revista:Journal of Medicinal Chemistry
Título revista abreviado:J. MED. CHEM.
ISSN:00222623
CODEN:JMCMA
CAS:Trypanocidal Agents
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v40_n15_p2314_Schvartzapel

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Citas:

---------- APA ----------
Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B. & Gros, E.G. (1997) . Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes). Journal of Medicinal Chemistry, 40(15), 2314-2322.
http://dx.doi.org/10.1021/jm9607616
---------- CHICAGO ----------
Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G. "Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)" . Journal of Medicinal Chemistry 40, no. 15 (1997) : 2314-2322.
http://dx.doi.org/10.1021/jm9607616
---------- MLA ----------
Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G. "Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)" . Journal of Medicinal Chemistry, vol. 40, no. 15, 1997, pp. 2314-2322.
http://dx.doi.org/10.1021/jm9607616
---------- VANCOUVER ----------
Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G. Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes). J. MED. CHEM. 1997;40(15):2314-2322.
http://dx.doi.org/10.1021/jm9607616