Antiinflammatory Activity of Triazine Thiazolidinone Derivatives: Molecular Docking and Pharmacophore Modeling
By: Shinde, R. S
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Contributor(s): Masand, V. H.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2019Edition: Vol. 81 (05).Description: 851-858p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: Some 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-phenylthiazolidin-4-one derivatives were prepared by cyclocondensation reaction between 2-amino-4,6-dichloro-1,3,5-triazine, substituted aromatic aldehyde and ethyl-2-mercaptoacetate, with an yield in the range 76-86 %. Prepared compounds showed antiinflammatory activity. The halogenated electron-withdrawing groups on the phenyl ring of 4-thiazolinone generated antiinflammatory activity. Among the synthesized compounds, 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-(2,5- difluorophenyl)thiazolidin-4-one showed better antiinflammatory activity with 72 and 79 % inhibition for TNF-α and IL-6, respectively. Also, molecular docking and pharmacophore modelling performed for this active antiinflammatory compound highlighted that hydrophobicity as an important feature for activity optimization.
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School of Pharmacy Archieval Section | Not for loan | 2020601 |
Some 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-phenylthiazolidin-4-one derivatives were prepared by cyclocondensation reaction between 2-amino-4,6-dichloro-1,3,5-triazine, substituted aromatic aldehyde and ethyl-2-mercaptoacetate, with an yield in the range 76-86 %. Prepared compounds showed antiinflammatory activity. The halogenated electron-withdrawing groups on the phenyl ring of 4-thiazolinone generated antiinflammatory activity. Among the synthesized compounds, 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-(2,5- difluorophenyl)thiazolidin-4-one showed better antiinflammatory activity with 72 and 79 % inhibition for TNF-α and IL-6, respectively. Also, molecular docking and pharmacophore modelling performed for this active antiinflammatory compound highlighted that hydrophobicity as an important feature for activity optimization.
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