Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)

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 antipro...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G.
Formato:	JOUR
Materias:	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
Acceso en línea:	http://hdl.handle.net/20.500.12110/paper_00222623_v40_n15_p2314_Schvartzapel
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

id	todo:paper_00222623_v40_n15_p2314_Schvartzapel
record_format	dspace
spelling	todo:paper_00222623_v40_n15_p2314_Schvartzapel2023-10-03T14:30:12Z Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes) Schvartzapel, A.J. Zhong, L. Docampo, R. Rodriguez, J.B. Gros, E.G. 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 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. Fil:Schvartzapel, A.J. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Rodriguez, J.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Gros, E.G. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00222623_v40_n15_p2314_Schvartzapel
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	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
spellingShingle	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 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)
topic_facet	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
description	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.
format	JOUR
author	Schvartzapel, A.J. Zhong, L. Docampo, R. Rodriguez, J.B. Gros, E.G.
author_facet	Schvartzapel, A.J. Zhong, L. Docampo, R. Rodriguez, J.B. Gros, E.G.
author_sort	Schvartzapel, A.J.
title	Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
title_short	Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
title_full	Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
title_fullStr	Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
title_full_unstemmed	Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
title_sort	design, synthesis, and biological evaluation of new growth inhibitors of trypanosoma cruzi (epimastigotes)
url	http://hdl.handle.net/20.500.12110/paper_00222623_v40_n15_p2314_Schvartzapel
work_keys_str_mv	AT schvartzapelaj designsynthesisandbiologicalevaluationofnewgrowthinhibitorsoftrypanosomacruziepimastigotes AT zhongl designsynthesisandbiologicalevaluationofnewgrowthinhibitorsoftrypanosomacruziepimastigotes AT docampor designsynthesisandbiologicalevaluationofnewgrowthinhibitorsoftrypanosomacruziepimastigotes AT rodriguezjb designsynthesisandbiologicalevaluationofnewgrowthinhibitorsoftrypanosomacruziepimastigotes AT groseg designsynthesisandbiologicalevaluationofnewgrowthinhibitorsoftrypanosomacruziepimastigotes
_version_	1807314465832566784

Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)

Ejemplares similares