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Synthesis and biological profile of substituted benzimidazoles

BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities. RESULTS AND DISCUSSION: The s...

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Autores principales: Vashist, Neelam, Sambi, Surinder Singh, Narasimhan, Balasubramanian, Kumar, Sanjiv, Lim, Siong Meng, Shah, Syed Adnan Ali, Ramasamy, Kalavathy, Mani, Vasudevan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768139/
https://www.ncbi.nlm.nih.gov/pubmed/30506405
http://dx.doi.org/10.1186/s13065-018-0498-y
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author Vashist, Neelam
Sambi, Surinder Singh
Narasimhan, Balasubramanian
Kumar, Sanjiv
Lim, Siong Meng
Shah, Syed Adnan Ali
Ramasamy, Kalavathy
Mani, Vasudevan
author_facet Vashist, Neelam
Sambi, Surinder Singh
Narasimhan, Balasubramanian
Kumar, Sanjiv
Lim, Siong Meng
Shah, Syed Adnan Ali
Ramasamy, Kalavathy
Mani, Vasudevan
author_sort Vashist, Neelam
collection PubMed
description BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities. RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug. CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC(50) values were more potent than 5-fluorouracil. [Image: see text]
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spelling pubmed-67681392019-10-03 Synthesis and biological profile of substituted benzimidazoles Vashist, Neelam Sambi, Surinder Singh Narasimhan, Balasubramanian Kumar, Sanjiv Lim, Siong Meng Shah, Syed Adnan Ali Ramasamy, Kalavathy Mani, Vasudevan Chem Cent J Research Article BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities. RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug. CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC(50) values were more potent than 5-fluorouracil. [Image: see text] Springer International Publishing 2018-12-01 /pmc/articles/PMC6768139/ /pubmed/30506405 http://dx.doi.org/10.1186/s13065-018-0498-y Text en © The Author(s) 2018 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Article
Vashist, Neelam
Sambi, Surinder Singh
Narasimhan, Balasubramanian
Kumar, Sanjiv
Lim, Siong Meng
Shah, Syed Adnan Ali
Ramasamy, Kalavathy
Mani, Vasudevan
Synthesis and biological profile of substituted benzimidazoles
title Synthesis and biological profile of substituted benzimidazoles
title_full Synthesis and biological profile of substituted benzimidazoles
title_fullStr Synthesis and biological profile of substituted benzimidazoles
title_full_unstemmed Synthesis and biological profile of substituted benzimidazoles
title_short Synthesis and biological profile of substituted benzimidazoles
title_sort synthesis and biological profile of substituted benzimidazoles
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768139/
https://www.ncbi.nlm.nih.gov/pubmed/30506405
http://dx.doi.org/10.1186/s13065-018-0498-y
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