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Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids
[Image: see text] A series of novel benzhydryl piperazine-coupled nitrobenzenesulfonamide hybrids were synthesized with good to excellent yields. They were tested for in vitro inhibition of mycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, in vitro cytotoxicity MTT (RAW 264...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2021
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8047747/ https://www.ncbi.nlm.nih.gov/pubmed/33869953 http://dx.doi.org/10.1021/acsomega.1c00369 |
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author | Murthy, Vallabhaneni S. Tamboli, Yasinalli Krishna, Vagolu Siva Sriram, Dharmarajan Zhang, Fang Xiong Zamponi, Gerald W. Vijayakumar, Vijayaparthasarathi |
author_facet | Murthy, Vallabhaneni S. Tamboli, Yasinalli Krishna, Vagolu Siva Sriram, Dharmarajan Zhang, Fang Xiong Zamponi, Gerald W. Vijayakumar, Vijayaparthasarathi |
author_sort | Murthy, Vallabhaneni S. |
collection | PubMed |
description | [Image: see text] A series of novel benzhydryl piperazine-coupled nitrobenzenesulfonamide hybrids were synthesized with good to excellent yields. They were tested for in vitro inhibition of mycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, in vitro cytotoxicity MTT (RAW 264.7cells) assay, nutrient starvation (H37Rv strain), and ability to block Cav3.2 T-type calcium channels. Novel hybrids did not inhibit T-type calcium channels, whereas they showed excellent antituberculosis (TB) activity and low cytotoxicity with a selectivity index of >30. A direct impact of the amino acid linker was not observed. Studied hybrids exhibited good inhibition activities, and the 2,4-dinitrobenzenesulfonamide group emerged as a promising scaffold for further drug design by hybridization approaches for anti-TB therapy. |
format | Online Article Text |
id | pubmed-8047747 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-80477472021-04-16 Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids Murthy, Vallabhaneni S. Tamboli, Yasinalli Krishna, Vagolu Siva Sriram, Dharmarajan Zhang, Fang Xiong Zamponi, Gerald W. Vijayakumar, Vijayaparthasarathi ACS Omega [Image: see text] A series of novel benzhydryl piperazine-coupled nitrobenzenesulfonamide hybrids were synthesized with good to excellent yields. They were tested for in vitro inhibition of mycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, in vitro cytotoxicity MTT (RAW 264.7cells) assay, nutrient starvation (H37Rv strain), and ability to block Cav3.2 T-type calcium channels. Novel hybrids did not inhibit T-type calcium channels, whereas they showed excellent antituberculosis (TB) activity and low cytotoxicity with a selectivity index of >30. A direct impact of the amino acid linker was not observed. Studied hybrids exhibited good inhibition activities, and the 2,4-dinitrobenzenesulfonamide group emerged as a promising scaffold for further drug design by hybridization approaches for anti-TB therapy. American Chemical Society 2021-03-31 /pmc/articles/PMC8047747/ /pubmed/33869953 http://dx.doi.org/10.1021/acsomega.1c00369 Text en © 2021 The Authors. Published by American Chemical Society Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Murthy, Vallabhaneni S. Tamboli, Yasinalli Krishna, Vagolu Siva Sriram, Dharmarajan Zhang, Fang Xiong Zamponi, Gerald W. Vijayakumar, Vijayaparthasarathi Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids |
title | Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled
Nitrobenzenesulfonamide Hybrids |
title_full | Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled
Nitrobenzenesulfonamide Hybrids |
title_fullStr | Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled
Nitrobenzenesulfonamide Hybrids |
title_full_unstemmed | Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled
Nitrobenzenesulfonamide Hybrids |
title_short | Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled
Nitrobenzenesulfonamide Hybrids |
title_sort | synthesis and biological evaluation of novel benzhydrylpiperazine-coupled
nitrobenzenesulfonamide hybrids |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8047747/ https://www.ncbi.nlm.nih.gov/pubmed/33869953 http://dx.doi.org/10.1021/acsomega.1c00369 |
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