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New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents

A novel series of dihydropyrimidines (DHPMs) 4a–j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on...

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Autores principales: Radini, Ibrahim Ali M., Elsheikh, Tarek M. Y., El-Telbani, Emad M., Khidre, Rizk E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273215/
https://www.ncbi.nlm.nih.gov/pubmed/27428939
http://dx.doi.org/10.3390/molecules21070909
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author Radini, Ibrahim Ali M.
Elsheikh, Tarek M. Y.
El-Telbani, Emad M.
Khidre, Rizk E.
author_facet Radini, Ibrahim Ali M.
Elsheikh, Tarek M. Y.
El-Telbani, Emad M.
Khidre, Rizk E.
author_sort Radini, Ibrahim Ali M.
collection PubMed
description A novel series of dihydropyrimidines (DHPMs) 4a–j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC(50) values ranging from 0.014–5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).
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spelling pubmed-62732152018-12-28 New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents Radini, Ibrahim Ali M. Elsheikh, Tarek M. Y. El-Telbani, Emad M. Khidre, Rizk E. Molecules Article A novel series of dihydropyrimidines (DHPMs) 4a–j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC(50) values ranging from 0.014–5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ). MDPI 2016-07-14 /pmc/articles/PMC6273215/ /pubmed/27428939 http://dx.doi.org/10.3390/molecules21070909 Text en © 2016 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 Article
Radini, Ibrahim Ali M.
Elsheikh, Tarek M. Y.
El-Telbani, Emad M.
Khidre, Rizk E.
New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title_full New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title_fullStr New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title_full_unstemmed New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title_short New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents
title_sort new potential antimalarial agents: design, synthesis and biological evaluation of some novel quinoline derivatives as antimalarial agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273215/
https://www.ncbi.nlm.nih.gov/pubmed/27428939
http://dx.doi.org/10.3390/molecules21070909
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