All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.

Abstract

Antiinflammatory Activity of Triazine Thiazolidinone Derivatives: Molecular Docking and Pharmacophore Modeling

Author(s): R. S. Shinde*, V. H. Masand1 and M. K. Patil2
Department of Chemistry, Dayanand Science College, Latur-413 512, 1Department of Chemistry, Vidya Bharati College, Amaravati-444 602, 2Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, Sub-Campus Osmanabad-413 501, India

Correspondence Address:
Department of Chemistry, Dayanand Science College, Latur-413 512, India, E-mail: rss.333@rediffmail.com


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.

Full-Text | PDF

 
 
Google scholar citation report
Citations : 69022

Indian Journal of Pharmaceutical Sciences received 69022 citations as per google scholar report