New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities

Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalaria...

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Main Authors: Barea, C. (Carlos), Pabon, A. (Adriana), Pérez-Silanes, S. (Silvia), Galiano, S. (Silvia), Gonzalez, G. (Germán), Monge, A. (Antonio), Deharo, E. (Eric), Aldana, I. (Ignacio)
Format: info:eu-repo/semantics/article
Language:eng
Published: MDPI 2013
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Online Access:https://hdl.handle.net/10171/29506
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author Barea, C. (Carlos)
Pabon, A. (Adriana)
Pérez-Silanes, S. (Silvia)
Galiano, S. (Silvia)
Gonzalez, G. (Germán)
Monge, A. (Antonio)
Deharo, E. (Eric)
Aldana, I. (Ignacio)
author_facet Barea, C. (Carlos)
Pabon, A. (Adriana)
Pérez-Silanes, S. (Silvia)
Galiano, S. (Silvia)
Gonzalez, G. (Germán)
Monge, A. (Antonio)
Deharo, E. (Eric)
Aldana, I. (Ignacio)
author_sort Barea, C. (Carlos)
collection DSpace
description Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 µM), while a cyclohexyl derivative (2.5 µM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 µM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position.
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spelling oai:dadun.unav.edu:10171-295062020-03-04T00:49:13Z New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities Barea, C. (Carlos) Pabon, A. (Adriana) Pérez-Silanes, S. (Silvia) Galiano, S. (Silvia) Gonzalez, G. (Germán) Monge, A. (Antonio) Deharo, E. (Eric) Aldana, I. (Ignacio) Quinoxaline 1,4-di-N-oxide Leishmanicidal Antiplasmodial Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 µM), while a cyclohexyl derivative (2.5 µM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 µM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position. 2013-07-18T07:54:43Z 2013-07-18T07:54:43Z 2013 info:eu-repo/semantics/article https://hdl.handle.net/10171/29506 eng info:eu-repo/semantics/openAccess application/pdf MDPI
spellingShingle Quinoxaline
1,4-di-N-oxide
Leishmanicidal
Antiplasmodial
Barea, C. (Carlos)
Pabon, A. (Adriana)
Pérez-Silanes, S. (Silvia)
Galiano, S. (Silvia)
Gonzalez, G. (Germán)
Monge, A. (Antonio)
Deharo, E. (Eric)
Aldana, I. (Ignacio)
New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title_full New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title_fullStr New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title_full_unstemmed New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title_short New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
title_sort new amide derivatives of quinoxaline 1,4-di-n-oxide with leishmanicidal and antiplasmodial activities
topic Quinoxaline
1,4-di-N-oxide
Leishmanicidal
Antiplasmodial
url https://hdl.handle.net/10171/29506
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