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Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates

The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates 6a-u w...

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Autores principales: Al-Wabli, Reem I., Alsulami, Mona A., Bukhari, Sarah I., Moubayed, Nadine M. S., Al-Mutairi, Maha S., Attia, Mohamed I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071222/
https://www.ncbi.nlm.nih.gov/pubmed/33920952
http://dx.doi.org/10.3390/molecules26082292
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author Al-Wabli, Reem I.
Alsulami, Mona A.
Bukhari, Sarah I.
Moubayed, Nadine M. S.
Al-Mutairi, Maha S.
Attia, Mohamed I.
author_facet Al-Wabli, Reem I.
Alsulami, Mona A.
Bukhari, Sarah I.
Moubayed, Nadine M. S.
Al-Mutairi, Maha S.
Attia, Mohamed I.
author_sort Al-Wabli, Reem I.
collection PubMed
description The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates 6a-u was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans.
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spelling pubmed-80712222021-04-26 Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates Al-Wabli, Reem I. Alsulami, Mona A. Bukhari, Sarah I. Moubayed, Nadine M. S. Al-Mutairi, Maha S. Attia, Mohamed I. Molecules Article The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates 6a-u was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans. MDPI 2021-04-15 /pmc/articles/PMC8071222/ /pubmed/33920952 http://dx.doi.org/10.3390/molecules26082292 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Al-Wabli, Reem I.
Alsulami, Mona A.
Bukhari, Sarah I.
Moubayed, Nadine M. S.
Al-Mutairi, Maha S.
Attia, Mohamed I.
Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title_full Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title_fullStr Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title_full_unstemmed Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title_short Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
title_sort design, synthesis, and antimicrobial activity of certain new indole-1,2,4 triazole conjugates
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071222/
https://www.ncbi.nlm.nih.gov/pubmed/33920952
http://dx.doi.org/10.3390/molecules26082292
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