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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Format: | info:eu-repo/semantics/article |
Language: | eng |
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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. |
format | info:eu-repo/semantics/article |
id | oai:dadun.unav.edu:10171-29506 |
institution | Universidad de Navarra |
language | eng |
publishDate | 2013 |
publisher | MDPI |
record_format | dspace |
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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