β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation

A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC(50) values o...

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Detalles Bibliográficos
Autores principales: Nisha, Gut, Jiri, Rosenthal, Philip J., Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2014
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115587/
https://www.ncbi.nlm.nih.gov/pubmed/25062007
http://dx.doi.org/10.1016/j.ejmech.2014.07.064
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author Nisha
Gut, Jiri
Rosenthal, Philip J.
Kumar, Vipan
author_facet Nisha
Gut, Jiri
Rosenthal, Philip J.
Kumar, Vipan
author_sort Nisha
collection PubMed
description A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC(50) values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.
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spelling pubmed-71155872020-04-02 β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation Nisha Gut, Jiri Rosenthal, Philip J. Kumar, Vipan Eur J Med Chem Short Communication A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC(50) values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity. Elsevier Masson SAS. 2014-09-12 2014-07-21 /pmc/articles/PMC7115587/ /pubmed/25062007 http://dx.doi.org/10.1016/j.ejmech.2014.07.064 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 Short Communication
Nisha
Gut, Jiri
Rosenthal, Philip J.
Kumar, Vipan
β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title_full β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title_fullStr β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title_full_unstemmed β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title_short β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation
title_sort β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115587/
https://www.ncbi.nlm.nih.gov/pubmed/25062007
http://dx.doi.org/10.1016/j.ejmech.2014.07.064
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