Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies

One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesi...

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Autores principales: Singh, Kamaljit, Kaur, Hardeep, Chibale, Kelly, Balzarini, Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2013
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115683/
https://www.ncbi.nlm.nih.gov/pubmed/23811093
http://dx.doi.org/10.1016/j.ejmech.2013.05.046
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author Singh, Kamaljit
Kaur, Hardeep
Chibale, Kelly
Balzarini, Jan
author_facet Singh, Kamaljit
Kaur, Hardeep
Chibale, Kelly
Balzarini, Jan
author_sort Singh, Kamaljit
collection PubMed
description One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.
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spelling pubmed-71156832020-04-02 Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies Singh, Kamaljit Kaur, Hardeep Chibale, Kelly Balzarini, Jan Eur J Med Chem Original Article One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA. Elsevier Masson SAS. 2013-08 2013-06-10 /pmc/articles/PMC7115683/ /pubmed/23811093 http://dx.doi.org/10.1016/j.ejmech.2013.05.046 Text en Copyright © 2013 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 Original Article
Singh, Kamaljit
Kaur, Hardeep
Chibale, Kelly
Balzarini, Jan
Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title_full Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title_fullStr Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title_full_unstemmed Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title_short Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
title_sort synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115683/
https://www.ncbi.nlm.nih.gov/pubmed/23811093
http://dx.doi.org/10.1016/j.ejmech.2013.05.046
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AT chibalekelly synthesisof4aminoquinolinepyrimidinehybridsaspotentantimalarialsandtheirmodeofactionstudies
AT balzarinijan synthesisof4aminoquinolinepyrimidinehybridsaspotentantimalarialsandtheirmodeofactionstudies

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