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Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments
Malaria is among the deadliest infectious diseases in the world caused by Plasmodium parasites. Due to the high complexity of the parasite’s life cycle, we partly depend on antimalarial drugs to fight this disease. However, the emergence of resistance, mainly by Plasmodium falciparum, has dethroned...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7865557/ https://www.ncbi.nlm.nih.gov/pubmed/33498868 http://dx.doi.org/10.3390/molecules26030600 |
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author | Fonte, Mélanie Tassi, Natália Gomes, Paula Teixeira, Cátia |
author_facet | Fonte, Mélanie Tassi, Natália Gomes, Paula Teixeira, Cátia |
author_sort | Fonte, Mélanie |
collection | PubMed |
description | Malaria is among the deadliest infectious diseases in the world caused by Plasmodium parasites. Due to the high complexity of the parasite’s life cycle, we partly depend on antimalarial drugs to fight this disease. However, the emergence of resistance, mainly by Plasmodium falciparum, has dethroned most of the antimalarials developed to date. Given recent reports of resistance to artemisinin combination therapies, first-line treatment currently recommended by the World Health Organization, in Western Cambodia and across the Greater Mekong sub-region, it seems very likely that artemisinin and its derivatives will follow the same path of other antimalarial drugs. Consequently, novel, safe and efficient antimalarial drugs are urgently needed. One fast and low-cost strategy to accelerate antimalarial development is by recycling classical pharmacophores. Quinacrine, an acridine-based compound and the first clinically tested synthetic antimalarial drug with potent blood schizonticide but serious side effects, has attracted attention due to its broad spectrum of biological activity. In this sense, the present review will focus on efforts made in the last 20 years for the development of more efficient, safer and affordable antimalarial compounds, through recycling the classical quinacrine drug. |
format | Online Article Text |
id | pubmed-7865557 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-78655572021-02-07 Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments Fonte, Mélanie Tassi, Natália Gomes, Paula Teixeira, Cátia Molecules Review Malaria is among the deadliest infectious diseases in the world caused by Plasmodium parasites. Due to the high complexity of the parasite’s life cycle, we partly depend on antimalarial drugs to fight this disease. However, the emergence of resistance, mainly by Plasmodium falciparum, has dethroned most of the antimalarials developed to date. Given recent reports of resistance to artemisinin combination therapies, first-line treatment currently recommended by the World Health Organization, in Western Cambodia and across the Greater Mekong sub-region, it seems very likely that artemisinin and its derivatives will follow the same path of other antimalarial drugs. Consequently, novel, safe and efficient antimalarial drugs are urgently needed. One fast and low-cost strategy to accelerate antimalarial development is by recycling classical pharmacophores. Quinacrine, an acridine-based compound and the first clinically tested synthetic antimalarial drug with potent blood schizonticide but serious side effects, has attracted attention due to its broad spectrum of biological activity. In this sense, the present review will focus on efforts made in the last 20 years for the development of more efficient, safer and affordable antimalarial compounds, through recycling the classical quinacrine drug. MDPI 2021-01-24 /pmc/articles/PMC7865557/ /pubmed/33498868 http://dx.doi.org/10.3390/molecules26030600 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Fonte, Mélanie Tassi, Natália Gomes, Paula Teixeira, Cátia Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title | Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title_full | Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title_fullStr | Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title_full_unstemmed | Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title_short | Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments |
title_sort | acridine-based antimalarials—from the very first synthetic antimalarial to recent developments |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7865557/ https://www.ncbi.nlm.nih.gov/pubmed/33498868 http://dx.doi.org/10.3390/molecules26030600 |
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