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Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives
Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Springer US
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9647759/ https://www.ncbi.nlm.nih.gov/pubmed/36405379 http://dx.doi.org/10.1007/s11094-022-02755-3 |
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author | Moharana, Alok Kumar Dash, Rudra Narayan Mahanandia, Nimai Charan Subudhi, Bharat Bhusan |
author_facet | Moharana, Alok Kumar Dash, Rudra Narayan Mahanandia, Nimai Charan Subudhi, Bharat Bhusan |
author_sort | Moharana, Alok Kumar |
collection | PubMed |
description | Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based drugs with wide range of applications. This study was undertaken to develop new small molecules with anti-inflammatory properties. Compounds MBPHYD, MBNHYD and MBHYDX were synthesised, purified, characterised and found to be non-toxic both in vitro (in 100 μMconcentration for 24 h vs. 3000 Vero cells/well) and in vivo (at a dose of 100 mg/kg in female Wistar rats with animals observed for 48 h for any mortality). Compounds MBPHYD and MBNHYD were found to possess significant anti-inflammatory properties. Further, in silico analysis suggested their compliance with drug-likeness. While no toxicity was predicted, both compounds were suggested to have good oral bioavailability. Thus, results of this study may encourage further investigation to establish new anti-inflammatory benzimidazoles for application against various disease conditions. |
format | Online Article Text |
id | pubmed-9647759 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Springer US |
record_format | MEDLINE/PubMed |
spelling | pubmed-96477592022-11-14 Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives Moharana, Alok Kumar Dash, Rudra Narayan Mahanandia, Nimai Charan Subudhi, Bharat Bhusan Pharm Chem J Article Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based drugs with wide range of applications. This study was undertaken to develop new small molecules with anti-inflammatory properties. Compounds MBPHYD, MBNHYD and MBHYDX were synthesised, purified, characterised and found to be non-toxic both in vitro (in 100 μMconcentration for 24 h vs. 3000 Vero cells/well) and in vivo (at a dose of 100 mg/kg in female Wistar rats with animals observed for 48 h for any mortality). Compounds MBPHYD and MBNHYD were found to possess significant anti-inflammatory properties. Further, in silico analysis suggested their compliance with drug-likeness. While no toxicity was predicted, both compounds were suggested to have good oral bioavailability. Thus, results of this study may encourage further investigation to establish new anti-inflammatory benzimidazoles for application against various disease conditions. Springer US 2022-11-10 2022 /pmc/articles/PMC9647759/ /pubmed/36405379 http://dx.doi.org/10.1007/s11094-022-02755-3 Text en © Springer Science+Business Media, LLC, part of Springer Nature 2022, Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic. |
spellingShingle | Article Moharana, Alok Kumar Dash, Rudra Narayan Mahanandia, Nimai Charan Subudhi, Bharat Bhusan Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title | Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title_full | Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title_fullStr | Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title_full_unstemmed | Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title_short | Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives |
title_sort | synthesis and anti-inflammatory activity evaluation of some benzimidazole derivatives |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9647759/ https://www.ncbi.nlm.nih.gov/pubmed/36405379 http://dx.doi.org/10.1007/s11094-022-02755-3 |
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