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Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents

A novel series of 4,6-disubstituted s-triazin-2-yl amino acid derivatives was prepared and characterized. Most of them showed antifungal activity against Candida albicans compared to clotrimazole (standard drug). Compounds bearing aniline derivatives, piperidine and glycine on the triazine core show...

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Autores principales: Abd Alhameed, Rakia, Almarhoon, Zainab, N. Sholkamy, Essam, Ali Khan, Salman, Ul-Haq, Zaheer, Sharma, Anamika, G. de la Torre, Beatriz, Albericio, Fernando, El-Faham, Ayman
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7712924/
https://www.ncbi.nlm.nih.gov/pubmed/33096851
http://dx.doi.org/10.3390/jof6040237
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author Abd Alhameed, Rakia
Almarhoon, Zainab
N. Sholkamy, Essam
Ali Khan, Salman
Ul-Haq, Zaheer
Sharma, Anamika
G. de la Torre, Beatriz
Albericio, Fernando
El-Faham, Ayman
author_facet Abd Alhameed, Rakia
Almarhoon, Zainab
N. Sholkamy, Essam
Ali Khan, Salman
Ul-Haq, Zaheer
Sharma, Anamika
G. de la Torre, Beatriz
Albericio, Fernando
El-Faham, Ayman
author_sort Abd Alhameed, Rakia
collection PubMed
description A novel series of 4,6-disubstituted s-triazin-2-yl amino acid derivatives was prepared and characterized. Most of them showed antifungal activity against Candida albicans compared to clotrimazole (standard drug). Compounds bearing aniline derivatives, piperidine and glycine on the triazine core showed the highest inhibition zones at concentrations of 50, 100, 200, and 300 μg per disc. In addition, docking studies revealed that all the compounds accommodated well in the active site residues of N-myristoltransferase (NMT) and exhibited complementarity, which explains the observed antifungal activity. Interestingly, none of these compounds showed antibacterial activity.
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spelling pubmed-77129242020-12-04 Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents Abd Alhameed, Rakia Almarhoon, Zainab N. Sholkamy, Essam Ali Khan, Salman Ul-Haq, Zaheer Sharma, Anamika G. de la Torre, Beatriz Albericio, Fernando El-Faham, Ayman J Fungi (Basel) Article A novel series of 4,6-disubstituted s-triazin-2-yl amino acid derivatives was prepared and characterized. Most of them showed antifungal activity against Candida albicans compared to clotrimazole (standard drug). Compounds bearing aniline derivatives, piperidine and glycine on the triazine core showed the highest inhibition zones at concentrations of 50, 100, 200, and 300 μg per disc. In addition, docking studies revealed that all the compounds accommodated well in the active site residues of N-myristoltransferase (NMT) and exhibited complementarity, which explains the observed antifungal activity. Interestingly, none of these compounds showed antibacterial activity. MDPI 2020-10-21 /pmc/articles/PMC7712924/ /pubmed/33096851 http://dx.doi.org/10.3390/jof6040237 Text en © 2020 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
Abd Alhameed, Rakia
Almarhoon, Zainab
N. Sholkamy, Essam
Ali Khan, Salman
Ul-Haq, Zaheer
Sharma, Anamika
G. de la Torre, Beatriz
Albericio, Fernando
El-Faham, Ayman
Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title_full Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title_fullStr Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title_full_unstemmed Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title_short Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents
title_sort novel 4,6-disubstituted s-triazin-2-yl amino acid derivatives as promising antifungal agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7712924/
https://www.ncbi.nlm.nih.gov/pubmed/33096851
http://dx.doi.org/10.3390/jof6040237
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