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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...

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Autores principales: Rezayan, Ali Hossein, Hariri, Safoura, Azerang, Parisa, Ghavami, Ghazaleh, Portugal, Isabel, Sardari, Soroush
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2017
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).
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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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