EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES

Parasitic infections such as leishmaniasis, trypanosomiasis and malaria have significant impacts in third world countries and are the major reasons of mortality. In order to search a new class of antiprotozoal agent, a series of ten quinolin-2-one derivatives was tested in vitro against the parasite...

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Autores principales:	Muscia,Gisela C, Bollini,Mariela, Bruno,Ana M, Asís,Silvia E
Lenguaje:	English
Publicado:	Sociedad Chilena de Química 2006
Materias:	3-Aminoquinolin-2-one Derivatives Angiogenesis Plasmodium falciparum Tuberculosis
Acceso en línea:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072006000200005
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spelling	oai:scielo:S0717-970720060002000052006-06-30EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVESMuscia,Gisela CBollini,MarielaBruno,Ana MAsís,Silvia E 3-Aminoquinolin-2-one Derivatives Angiogenesis Plasmodium falciparum Tuberculosis Parasitic infections such as leishmaniasis, trypanosomiasis and malaria have significant impacts in third world countries and are the major reasons of mortality. In order to search a new class of antiprotozoal agent, a series of ten quinolin-2-one derivatives was tested in vitro against the parasites causative of malaria, leishmaniasis, sleeping sickness and Chagas´ disease. In general, these compounds exhibited moderate activity against Plasmodium falciparum and showed no activity against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei. Facing to establish a possible mechanism of antimalarial activity their binding to hemin was assayed. Furthermore, the need of developing new therapeutic strategies for the effective control of tuberculosis prompted us to assay twelve of these compounds against Mycobacterium tuberculosis but they did not demonstrate inhibitory activity. In addition, three terms resulted also structurally related to linomide, a recognized drug against angiogenesis, an interesting target for designing new antineoplastic agents. So these compounds were selected at the National Cancer Institute for angiogenesis testing and they exhibited similar activity to those recently reported for linomide and its analoguesinfo:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.51 n.2 20062006-06-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072006000200005en10.4067/S0717-97072006000200005
institution	Scielo Chile
collection	Scielo Chile
language	English
topic	3-Aminoquinolin-2-one Derivatives Angiogenesis Plasmodium falciparum Tuberculosis
spellingShingle	3-Aminoquinolin-2-one Derivatives Angiogenesis Plasmodium falciparum Tuberculosis Muscia,Gisela C Bollini,Mariela Bruno,Ana M Asís,Silvia E EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
description	Parasitic infections such as leishmaniasis, trypanosomiasis and malaria have significant impacts in third world countries and are the major reasons of mortality. In order to search a new class of antiprotozoal agent, a series of ten quinolin-2-one derivatives was tested in vitro against the parasites causative of malaria, leishmaniasis, sleeping sickness and Chagas´ disease. In general, these compounds exhibited moderate activity against Plasmodium falciparum and showed no activity against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei. Facing to establish a possible mechanism of antimalarial activity their binding to hemin was assayed. Furthermore, the need of developing new therapeutic strategies for the effective control of tuberculosis prompted us to assay twelve of these compounds against Mycobacterium tuberculosis but they did not demonstrate inhibitory activity. In addition, three terms resulted also structurally related to linomide, a recognized drug against angiogenesis, an interesting target for designing new antineoplastic agents. So these compounds were selected at the National Cancer Institute for angiogenesis testing and they exhibited similar activity to those recently reported for linomide and its analogues
author	Muscia,Gisela C Bollini,Mariela Bruno,Ana M Asís,Silvia E
author_facet	Muscia,Gisela C Bollini,Mariela Bruno,Ana M Asís,Silvia E
author_sort	Muscia,Gisela C
title	EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
title_short	EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
title_full	EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
title_fullStr	EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
title_full_unstemmed	EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES
title_sort	evaluation of antiparasitic, antituberculosis and antiangiogenic activities of 3-aminoquinolin-2-one derivatives
publisher	Sociedad Chilena de Química
publishDate	2006
url	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072006000200005
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EVALUATION OF ANTIPARASITIC, ANTITUBERCULOSIS AND ANTIANGIOGENIC ACTIVITIES OF 3-AMINOQUINOLIN-2-ONE DERIVATIVES

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