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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...

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Detalles Bibliográficos
Autores principales: Srikanth Kumar, K., Lakshmana Rao, A., Basaveswara Rao, M.V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2018
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.
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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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