1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawin...

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Autores principales: Kumar, Kewal, Pradines, Bruno, Madamet, Marilyn, Amalvict, Rémy, Benoit, Nicolas, Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126053/
https://www.ncbi.nlm.nih.gov/pubmed/25440881
http://dx.doi.org/10.1016/j.ejmech.2014.10.024
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author Kumar, Kewal
Pradines, Bruno
Madamet, Marilyn
Amalvict, Rémy
Benoit, Nicolas
Kumar, Vipan
author_facet Kumar, Kewal
Pradines, Bruno
Madamet, Marilyn
Amalvict, Rémy
Benoit, Nicolas
Kumar, Vipan
author_sort Kumar, Kewal
collection PubMed
description 1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC(50) values of 3.76 and 4.58 μM against 3D7 and W2 strains, respectively.
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spelling pubmed-71260532020-04-08 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation Kumar, Kewal Pradines, Bruno Madamet, Marilyn Amalvict, Rémy Benoit, Nicolas Kumar, Vipan Eur J Med Chem Article 1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC(50) values of 3.76 and 4.58 μM against 3D7 and W2 strains, respectively. Elsevier Masson SAS. 2014-11-24 2014-10-13 /pmc/articles/PMC7126053/ /pubmed/25440881 http://dx.doi.org/10.1016/j.ejmech.2014.10.024 Text en Copyright © 2014 Elsevier Masson SAS. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Kumar, Kewal
Pradines, Bruno
Madamet, Marilyn
Amalvict, Rémy
Benoit, Nicolas
Kumar, Vipan
1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title_full 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title_fullStr 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title_full_unstemmed 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title_short 1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation
title_sort 1h-1,2,3-triazole tethered isatin-ferrocene conjugates: synthesis and in vitro antimalarial evaluation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126053/
https://www.ncbi.nlm.nih.gov/pubmed/25440881
http://dx.doi.org/10.1016/j.ejmech.2014.10.024
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