Abstract

DESIGN AND SYNTHESIS OF NOVEL PPART AGONISTS: ENHANCING INSULIN SENSITIVITY THROUGH THE INCORPORATION OF ACIDIC AND AROMATIC AMINO ACIDS IN PLACE OF PYRIDINE RING IN ROSIGLITAZONE DERIVATIVES

Anant Nag Gautam*, Rajeev Sahai, Manoj Kumar, Atul Kumar, Laxmi Devi Gangwar

Abstract

Heterocyclic compounds are organic compounds that contain at least one atom other than carbon within a ring structure. These compounds are incredibly important in medicinal chemistry because they often exhibit a wide range of biological activities, making them useful in the treatment of various diseases. Rosiglitazone is a member of the thiazolidinedione (TZD) class of drugs, which are primarily used to improve insulin sensitivity in the treatment of type 2 diabetes mellitus. The structure-activity relationship (SAR) of Rosiglitazone can be understood by analyzing the key structural components of the molecule and how they contribute to its biological activity, particularly its role as a selective agonist for the peroxisome proliferator- activated receptor gamma (PPARγ).Peroxisome proliferator-activated receptor gamma (PPARγ) is a type of nuclear receptor that functions as a transcription factor, regulating the expression of specific genes involved in various metabolic processes. PPARγ plays a crucial role in the regulation of glucose metabolism, lipid metabolism, and adipogenesis (the formation of fat cells). It is particularly important in the context of insulin sensitivity and the development of type 2 diabetes. Lipophilicity refers to the chemical property of a substance that describes its ability to dissolve in fats, oils, and nonpolar solvents, such as organic solvents (e.g., hexane or chloroform). In simpler terms, it is the affinity of a molecule for a lipid environment over an aqueous (water) environment. Lipophilic substances are typically non-polar or have significant non-polar regions, which makes them more soluble in lipids than in water.

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