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Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives
Various thiazolidine-2,4-dione derivatives 3a-l possessing indole moiety were designed, synthesized using appropriate conventional heating as well as microwave irradiation methods. All the synthesized compounds were characterized physically and spectrally. The compounds were evaluated for in vitro a...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6154471/ https://www.ncbi.nlm.nih.gov/pubmed/30258996 http://dx.doi.org/10.1016/j.heliyon.2018.e00807 |
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author | Srikanth Kumar, K. Lakshmana Rao, A. Basaveswara Rao, M.V. |
author_facet | Srikanth Kumar, K. Lakshmana Rao, A. Basaveswara Rao, M.V. |
author_sort | Srikanth Kumar, K. |
collection | PubMed |
description | Various thiazolidine-2,4-dione derivatives 3a-l possessing indole moiety were designed, synthesized using appropriate conventional heating as well as microwave irradiation methods. All the synthesized compounds were characterized physically and spectrally. The compounds were evaluated for in vitro antibacterial activity, in vitro antioxidant activity and in vivo hypoglycemic activity in relation to the standard drugs. Most of the new compounds exhibited moderate activity and some showed considerable activity. Molecular docking studies were carried out using AutoDock software and revealed that compound 3b has significant binding interaction with PPARγ receptor compared with the standard ligand Rosiglitazone. |
format | Online Article Text |
id | pubmed-6154471 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-61544712018-09-26 Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives Srikanth Kumar, K. Lakshmana Rao, A. Basaveswara Rao, M.V. Heliyon Article Various thiazolidine-2,4-dione derivatives 3a-l possessing indole moiety were designed, synthesized using appropriate conventional heating as well as microwave irradiation methods. All the synthesized compounds were characterized physically and spectrally. The compounds were evaluated for in vitro antibacterial activity, in vitro antioxidant activity and in vivo hypoglycemic activity in relation to the standard drugs. Most of the new compounds exhibited moderate activity and some showed considerable activity. Molecular docking studies were carried out using AutoDock software and revealed that compound 3b has significant binding interaction with PPARγ receptor compared with the standard ligand Rosiglitazone. Elsevier 2018-09-20 /pmc/articles/PMC6154471/ /pubmed/30258996 http://dx.doi.org/10.1016/j.heliyon.2018.e00807 Text en © 2018 Published by Elsevier Ltd. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Article Srikanth Kumar, K. Lakshmana Rao, A. Basaveswara Rao, M.V. Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title | Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title_full | Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title_fullStr | Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title_full_unstemmed | Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title_short | Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
title_sort | design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6154471/ https://www.ncbi.nlm.nih.gov/pubmed/30258996 http://dx.doi.org/10.1016/j.heliyon.2018.e00807 |
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