Asian Journal of Pharmaceutical Research

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

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


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

   Subscribe/Renew Journal


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.
Subscription Login to verify subscription
User
Notifications
Font Size


  • Baynes J Diabetes Metab (2015) Volume 6, Journal of diabetes and metabolism.

  • Rang HP, Dale MM, Ritter JM, Moore PK.(2007),rang and dale pharmacology china: Churchill livingstone.6th edition p.402-408

  • Mark S. (2003), Insulin and hypoglycemic agents, Abraham DJ. Bergers medicinal chemistry and drug discovery. Vol.4 6th edition. united states of America :john wiley and sons inc p.1-37

  • Mcgrady, Angele, James H. (1999), Coplementary/Alternative therapies in General medicine: diabetes mellitus.john WS and Joseph jj. Comple/alterna medicine: an evidence based approach.st.louis,mosby

  • Donald McClain, Animal Models of Diabetic Complications Consortium Intraperitoneal Glucose Tolerance Testing (IPGTT) Version: 1.0


Abstract Views: 563

PDF Views: 0




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

Abstract Views: 563  |  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