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Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species
A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5603884/ https://www.ncbi.nlm.nih.gov/pubmed/29118816 |
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author | Rezayan, Ali Hossein Hariri, Safoura Azerang, Parisa Ghavami, Ghazaleh Portugal, Isabel Sardari, Soroush |
author_facet | Rezayan, Ali Hossein Hariri, Safoura Azerang, Parisa Ghavami, Ghazaleh Portugal, Isabel Sardari, Soroush |
author_sort | Rezayan, Ali Hossein |
collection | PubMed |
description | A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done. These compounds were evaluated as anti-bacterial agents against Mycobacterium bovis and M. tuberculosis, while their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Among the twenty-three synthesized compounds, 5a was found to be the most active compound in vitro with MIC of 1.95 μg/mL against Mycobactrium bovis and compound 5k showed greatest potency against sensitive and resistant strains of M. tuberculosis (H37Rv, IHMT149/09, HPV115/08, and HPV65/08). |
format | Online Article Text |
id | pubmed-5603884 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-56038842017-11-08 Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species Rezayan, Ali Hossein Hariri, Safoura Azerang, Parisa Ghavami, Ghazaleh Portugal, Isabel Sardari, Soroush Iran J Pharm Res Original Article A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done. These compounds were evaluated as anti-bacterial agents against Mycobacterium bovis and M. tuberculosis, while their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Among the twenty-three synthesized compounds, 5a was found to be the most active compound in vitro with MIC of 1.95 μg/mL against Mycobactrium bovis and compound 5k showed greatest potency against sensitive and resistant strains of M. tuberculosis (H37Rv, IHMT149/09, HPV115/08, and HPV65/08). Shaheed Beheshti University of Medical Sciences 2017 /pmc/articles/PMC5603884/ /pubmed/29118816 Text en © 2017 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Article Rezayan, Ali Hossein Hariri, Safoura Azerang, Parisa Ghavami, Ghazaleh Portugal, Isabel Sardari, Soroush Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title | Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title_full | Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title_fullStr | Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title_full_unstemmed | Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title_short | Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species |
title_sort | synthesis of novel fluorene bisamide derivatives via ugi reaction and evaluation their biological activity against mycobacterium species |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5603884/ https://www.ncbi.nlm.nih.gov/pubmed/29118816 |
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