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Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents
Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the doc...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Hindawi Publishing Corporation
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4334925/ https://www.ncbi.nlm.nih.gov/pubmed/25734015 http://dx.doi.org/10.1155/2015/670181 |
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author | Datar, Prasanna A. Jadhav, Sonali R. |
author_facet | Datar, Prasanna A. Jadhav, Sonali R. |
author_sort | Datar, Prasanna A. |
collection | PubMed |
description | Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard. Compound 4 having sulphonamide derivative was found to be the most potent compound among the series. |
format | Online Article Text |
id | pubmed-4334925 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Hindawi Publishing Corporation |
record_format | MEDLINE/PubMed |
spelling | pubmed-43349252015-03-02 Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents Datar, Prasanna A. Jadhav, Sonali R. Int J Med Chem Research Article Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard. Compound 4 having sulphonamide derivative was found to be the most potent compound among the series. Hindawi Publishing Corporation 2015 2015-02-04 /pmc/articles/PMC4334925/ /pubmed/25734015 http://dx.doi.org/10.1155/2015/670181 Text en Copyright © 2015 P. A. Datar and S. R. Jadhav. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Datar, Prasanna A. Jadhav, Sonali R. Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title | Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title_full | Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title_fullStr | Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title_full_unstemmed | Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title_short | Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents |
title_sort | design and synthesis of pyrazole-3-one derivatives as hypoglycaemic agents |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4334925/ https://www.ncbi.nlm.nih.gov/pubmed/25734015 http://dx.doi.org/10.1155/2015/670181 |
work_keys_str_mv | AT datarprasannaa designandsynthesisofpyrazole3onederivativesashypoglycaemicagents AT jadhavsonalir designandsynthesisofpyrazole3onederivativesashypoglycaemicagents |