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In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives

BACKGROUND: Malaria is a neglected tropical parasitic disease affecting billons of people around the globe. Though the number of cases and deaths associated with malaria are decreasing in recent years, it is the most deadly disease in the world. This study aimed at investigating the in vivo antimala...

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Autores principales: Birhan, Yihenew Simegniew, Bekhit, Adnan Ahmed, Hymete, Ariaya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4617912/
https://www.ncbi.nlm.nih.gov/pubmed/26486987
http://dx.doi.org/10.1186/s13104-015-1578-x
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author Birhan, Yihenew Simegniew
Bekhit, Adnan Ahmed
Hymete, Ariaya
author_facet Birhan, Yihenew Simegniew
Bekhit, Adnan Ahmed
Hymete, Ariaya
author_sort Birhan, Yihenew Simegniew
collection PubMed
description BACKGROUND: Malaria is a neglected tropical parasitic disease affecting billons of people around the globe. Though the number of cases and deaths associated with malaria are decreasing in recent years, it is the most deadly disease in the world. This study aimed at investigating the in vivo antimalarial activities of some 2,3-disubstituted-4(3H)-quinazolinone derivatives. RESULTS: The in vivo antimalarial activities of the test compounds (6–9 and 11–13) were investigated using the 4-day suppressive standard test in mice infected with chloroquine-sensitive Plasmodium berghei ANKA strain. The tested compounds showed significant antimalarial activities with mean percentage suppression of 43.71–72.86 % which is significantly higher than the negative control group (p < 0.05). Compounds 12 and 13 displayed better antimalarial activities from the group with mean percentage suppression of 67.60 and 72.86 % respectively. CONCLUSION: The tested compounds showed significant in vivo antimalarial activities in mice infected with P. berghi ANKA strain. Thus, 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones represent a possible scaffold for the development of antimalarial agents.
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spelling pubmed-46179122015-10-25 In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives Birhan, Yihenew Simegniew Bekhit, Adnan Ahmed Hymete, Ariaya BMC Res Notes Research Article BACKGROUND: Malaria is a neglected tropical parasitic disease affecting billons of people around the globe. Though the number of cases and deaths associated with malaria are decreasing in recent years, it is the most deadly disease in the world. This study aimed at investigating the in vivo antimalarial activities of some 2,3-disubstituted-4(3H)-quinazolinone derivatives. RESULTS: The in vivo antimalarial activities of the test compounds (6–9 and 11–13) were investigated using the 4-day suppressive standard test in mice infected with chloroquine-sensitive Plasmodium berghei ANKA strain. The tested compounds showed significant antimalarial activities with mean percentage suppression of 43.71–72.86 % which is significantly higher than the negative control group (p < 0.05). Compounds 12 and 13 displayed better antimalarial activities from the group with mean percentage suppression of 67.60 and 72.86 % respectively. CONCLUSION: The tested compounds showed significant in vivo antimalarial activities in mice infected with P. berghi ANKA strain. Thus, 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones represent a possible scaffold for the development of antimalarial agents. BioMed Central 2015-10-20 /pmc/articles/PMC4617912/ /pubmed/26486987 http://dx.doi.org/10.1186/s13104-015-1578-x Text en © Birhan et al. 2015 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Article
Birhan, Yihenew Simegniew
Bekhit, Adnan Ahmed
Hymete, Ariaya
In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title_full In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title_fullStr In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title_full_unstemmed In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title_short In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
title_sort in vivo antimalarial evaluation of some 2,3-disubstituted-4(3h)-quinazolinone derivatives
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4617912/
https://www.ncbi.nlm.nih.gov/pubmed/26486987
http://dx.doi.org/10.1186/s13104-015-1578-x
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