Structure–activity relationships of pancreatic α-amylase and α-glucosidase as antidiabetic targets

Autor: Ameeta RaviKumar, Sudha Ramkumar, Prasad D Dandekar
Rok vydání: 2021
Předmět:
Zdroj: Bioactive Natural Products ISBN: 9780128194898
Popis: Diabetes mellitus is a complex metabolic disorder characterized by impaired glucose homeostasis and hyperglycemia. Its pathophysiology and progression are determined by genetic and environmental factors. Prolonged hyperglycemia causes abnormalities of vital organs; hence, its reduction is an important therapeutic goal. Pancreatic α-amylase and α-glucosidase activities correlate to postprandial hyperglycemia (PPHG); hence, their reduction using inhibitors is important. Current therapies, although effective, have limitations and demand safer alternatives. In this context, bioactive natural products have been reported to exhibit potent amylase and glucosidase inhibition. However, limitations exist in terms of their bioavailability and very few studies have explored their mechanistic insight. Structure–activity relationship (SAR) allows designing of molecules with improved activity through understanding relationship between chemical structures and biological activity. SAR is key to many aspects of drug discovery, ranging from primary screening to lead optimization. This chapter explores the available literature for advances in amylase and glucosidase inhibitors from natural sources and their SARs.
Databáze: OpenAIRE