Asian Journal of Pharmaceutical Research

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Computational Studies And Synthesis of Few Thiazolidine-2,4-Dion Analogues for Peroxisome Proliferator Activator Receptor- Γ Agonist as useful Antidiabetic Agent


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1 Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Nasik, Maharashtra, India
     

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Peroxisome proliferator activated receptor (PPAR)-γ is a member of the nuclear hormone receptor super family and the molecular target for the Thiazolidinediones (TZD), used clinically to treat insulin resistance in patients with type 2 diabetes. In addition to their efficacy to improve insulin sensitivity. Diabetes mellitus is a metabolic disease characterized by the presence of chronic hyperglycemia accompanied by greater or lesser impairment in the metabolism of carbohydrates, proteins and lipids. The present work shows the rational design of some novel PPAR-γ agonists involving computational study performed by Molecular Design Suite (MDS) in to ligand binding domain of PPAR-γ receptor to explore conformations of molecules. The compounds synthesized using multi-step synthesis protocol. The purity of synthesized compound was ascertained by IR, NMR, Mass and elemental analysis and tested by oral glucose tolerance test (OGTT). Two molecules showed most prominent activity on hyperglycemic control.

Keywords

Diabetic Mellitus, Thiazolidinedione, Computational Study.
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  • Computational Studies And Synthesis of Few Thiazolidine-2,4-Dion Analogues for Peroxisome Proliferator Activator Receptor- Γ Agonist as useful Antidiabetic Agent

Abstract Views: 463  |  PDF Views: 0

Authors

Shital N. Chaskar
Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Nasik, Maharashtra, India
Sanjay J. Kshirsagar
Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Nasik, Maharashtra, India

Abstract


Peroxisome proliferator activated receptor (PPAR)-γ is a member of the nuclear hormone receptor super family and the molecular target for the Thiazolidinediones (TZD), used clinically to treat insulin resistance in patients with type 2 diabetes. In addition to their efficacy to improve insulin sensitivity. Diabetes mellitus is a metabolic disease characterized by the presence of chronic hyperglycemia accompanied by greater or lesser impairment in the metabolism of carbohydrates, proteins and lipids. The present work shows the rational design of some novel PPAR-γ agonists involving computational study performed by Molecular Design Suite (MDS) in to ligand binding domain of PPAR-γ receptor to explore conformations of molecules. The compounds synthesized using multi-step synthesis protocol. The purity of synthesized compound was ascertained by IR, NMR, Mass and elemental analysis and tested by oral glucose tolerance test (OGTT). Two molecules showed most prominent activity on hyperglycemic control.

Keywords


Diabetic Mellitus, Thiazolidinedione, Computational Study.

References