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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Springer International Publishing
2018
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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] |
format | Online Article Text |
id | pubmed-6768139 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Springer International Publishing |
record_format | MEDLINE/PubMed |
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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