Protein Tyrosine Phosphatase1B (PTP1B) Inhibitor For The Treatment Of Diabetes, Obesity And Cancer:Carbohydrate-Based Mimetic In Drug Design

As we are aware, protein tyrosine phosphatase1B (PTP-1B) is a negative regulator of insulin receptor signaling and necessary drug target for the treatment of insulin resistance associated diabetes and obesity. In this research we depict the design, synthetic and related procedures for the prediction of the activities and binding modes of small molecule inhibitors toward the therapeutic target, protein tyrosine phosphatase1B (PTP1B). Designing molecules inhibiting the enzymatic function of PTP1B is of great medicinal interest. The research was done in three major sections and each containing its specified objectives.1. The first work stresses on the application of1-methoxy-O-glucoside as the central scaffold, where as salicylic pharmacophores were introduced with difference spatial arrangements probing into the structural preference of an enzymatic target, that is, protein tyrosine phosphatase1B (PTP-1B). With the employment of regioselective protection and deprotection strategies,2,6-,3,4-,4,6-, and2,3-di-O-propynyl-l-methoxy-O-glucosides were previously synthesized and coupled with azido salicylate glucosides with high yields.2. The second work emphasized on the preparation of glycosyl aminoxy acids as novel sugar building blocks and their further chemical and biological applications. Herein, carboxylic acid and amine functional groups were incorporated onto the sugar fragment that has widely been employed as carbohydrate scaffolds for the synthesis of carbohydrate-based molecules. These functional groups were introduced onto the C-3and C-4of the sugar fragment.3. And the purpose of the last work is to introduce the carboxylic acid functional group on to C-6of the pyranose ring and phospho-tyrosine (pTyr) mimetic on to the anomeric carbon of the sugar fragment. We also synthesized triazolyl sugar derivatives based on sugar aryl carboxylic acid hybrid using click chemistry. This research also seeks to synthesize and characterize protein tyrosine phosphatase1B inhibitor, using sugar amino acids and carbohydrates scaffolds, develop sugar amino acids building blocks, as central units for preparing novel protein tyrosine phosphatase1B (PTP1B) inhibitor and create bioactive molecule of the sugar template.