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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...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7712924 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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