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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| Format: | Article |
| Language: | English |
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Elsevier
2018-09-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844018322096 |
| _version_ | 1819014236285698048 |
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| author | K. Srikanth Kumar A. Lakshmana Rao M.V. Basaveswara Rao |
| author_facet | K. Srikanth Kumar A. Lakshmana Rao M.V. Basaveswara Rao |
| author_sort | K. Srikanth Kumar |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-21T02:12:38Z |
| format | Article |
| id | doaj.art-0b4416792bf8463f884b36338f15ce78 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-12-21T02:12:38Z |
| publishDate | 2018-09-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-0b4416792bf8463f884b36338f15ce782022-12-21T19:19:19ZengElsevierHeliyon2405-84402018-09-0149e00807Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivativesK. Srikanth Kumar0A. Lakshmana Rao1M.V. Basaveswara Rao2Department of Pharmaceutical Chemistry, V. V. Institute of Pharmaceutical Sciences, Gudlavalleru 521356, Andhra Pradesh, IndiaDepartment of Pharmaceutical Chemistry, V. V. Institute of Pharmaceutical Sciences, Gudlavalleru 521356, Andhra Pradesh, India; Corresponding author.Department of Chemistry, Krishna University, Machilipatnam 521002, Andhra Pradesh, IndiaVarious 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.http://www.sciencedirect.com/science/article/pii/S2405844018322096Pharmaceutical chemistry |
| spellingShingle | K. Srikanth Kumar A. Lakshmana Rao M.V. Basaveswara Rao Design, synthesis, biological evaluation and molecular docking studies of novel 3-substituted-5-[(indol-3-yl)methylene]-thiazolidine-2,4-dione derivatives Heliyon Pharmaceutical chemistry |
| 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 | Pharmaceutical chemistry |
| url | http://www.sciencedirect.com/science/article/pii/S2405844018322096 |
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