Design and Synthesis of Novel Compounds as Therapeutic Agents

Download or read book Design and Synthesis of Novel Compounds as Therapeutic Agents written by Mariam S. Shafqat and published by . This book was released on 2023 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Novel chemical moieties have been developed using structure-based drug design for the treatment of type 1 diabetes mellitus and cancer. In my first project, I studied novel small molecules for type 1 diabetes. Diabetes is an incurable, lifetime disease affecting millions of people worldwide. Our collaborators identified that the commercially available hydrazone moiety, EPB-1, increases insulin secretion while simultaneously protecting against pancreatic cell death making it a dual-function drug specifically targeted for type 1 diabetes. This compound’s unique dual-functional bioactivity has led us to explore hydrazones and other small molecules to uncover a new lead compound via structure-based drug design. A total of three generations of compounds have been synthesized and evaluated to identify the indazole-based amide, MSB-61, as a more potent analog making it our current lead compound. My second project investigates natural product-based analogs as potential anticancer agents. Natural products are an underexplored class of compounds with hidden potential. The commercially available, cheap raw material Stevioside is subjected to acid hydrolysis to isolate the natural product isosteviol. The skeletally diverse and stereochemically complex isosteviol scaffold has been used as the backbone to design analogs that exhibit a broad range of bioactivity including antimicrobial, antituberculosis, and cardioprotective properties. This research focuses on utilizing organic. synthetic techniques, such as the multicomponent Ugi reaction, to design and generate a compound library of isosteviol-based analogs as anticancer agents.