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Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine
Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical proper...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6696115/ https://www.ncbi.nlm.nih.gov/pubmed/31344947 http://dx.doi.org/10.3390/molecules24152696 |
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author | Teran, Rommy Guevara, Rommel Mora, Jessica Dobronski, Lizeth Barreiro-Costa, Olalla Beske, Timo Pérez-Barrera, Jorge Araya-Maturana, Ramiro Rojas-Silva, Patricio Poveda, Ana Heredia-Moya, Jorge |
author_facet | Teran, Rommy Guevara, Rommel Mora, Jessica Dobronski, Lizeth Barreiro-Costa, Olalla Beske, Timo Pérez-Barrera, Jorge Araya-Maturana, Ramiro Rojas-Silva, Patricio Poveda, Ana Heredia-Moya, Jorge |
author_sort | Teran, Rommy |
collection | PubMed |
description | Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded. |
format | Online Article Text |
id | pubmed-6696115 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-66961152019-09-05 Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine Teran, Rommy Guevara, Rommel Mora, Jessica Dobronski, Lizeth Barreiro-Costa, Olalla Beske, Timo Pérez-Barrera, Jorge Araya-Maturana, Ramiro Rojas-Silva, Patricio Poveda, Ana Heredia-Moya, Jorge Molecules Article Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded. MDPI 2019-07-24 /pmc/articles/PMC6696115/ /pubmed/31344947 http://dx.doi.org/10.3390/molecules24152696 Text en © 2019 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 Teran, Rommy Guevara, Rommel Mora, Jessica Dobronski, Lizeth Barreiro-Costa, Olalla Beske, Timo Pérez-Barrera, Jorge Araya-Maturana, Ramiro Rojas-Silva, Patricio Poveda, Ana Heredia-Moya, Jorge Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title | Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title_full | Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title_fullStr | Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title_full_unstemmed | Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title_short | Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine |
title_sort | characterization of antimicrobial, antioxidant, and leishmanicidal activities of schiff base derivatives of 4-aminoantipyrine |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6696115/ https://www.ncbi.nlm.nih.gov/pubmed/31344947 http://dx.doi.org/10.3390/molecules24152696 |
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