An insight on medicinal attributes of 1,2,3-and 1,2,4-triazole derivatives as alpha-amylase and alpha-glucosidase inhibitors

Diabetes Mellitus (DM) is the globe's common leading disease which is caused by high consumption of glucose. DM compiles groups of metabolic disorders which are characterized by inadequate secretion of insulin from pancreas, resulting in hyperglycemia condition. Many enzymes play a vital role in the metabolism of carbohydrate known as a-amylase and a-glucosidase which is calcium metalloenzyme that leads to breakdown of complex polysaccharides into glucose. To tackle this problem, search for newer antidiabetic drugs is the utmost need for the treatment and/or management of increasing diabetic burden. The inhibition of a-amylase and a-glucosidase is one of the effective therapeutic approaches for the development of antidiabetic therapeutics. The exhaustive literature survey has shown the importance of medicinally privileged triazole specifically 1,2,3-triazol and 1,2,4-triazoles scaffold tethered, fused and/ or clubbed with other heterocyclic rings structures as promising agents for designing and development of novel antidiabetic therapeutics. Molecular hybrids namely pyridazine-triazole, pyrazoline-triazole, benzothiazole-triazole, benzimidazole-triazole, curcumin-triazole, (bis) coumarin- triazole, acridine-9-carboxamide linked triazole, quinazolinone-triazole, xanthone-triazole, thiazolo-triazole, thiosemicarbazide-triazole, and indole clubbed-triazole are few examples which have shown promising antidiabetic activity by inhibiting a-amylase and/or a-glucosidase. The present review summarizes the structure-activity relationship ( SAR), enzyme inhibitory activity including IC50 values, percentage inhibition, kinetic studies, molecular docking studies, and patents filed of the both scaffolds as alpha-amylase and alpha-glucosidase inhibitors, which may be used for further development of potent inhibitors against both enzymes.

Automated summary

Diabetes Mellitus (DM) is a common global disease caused by high glucose consumption. Inhibiting enzymes such as α-amylase and α-glucosidase is an effective therapeutic approach for the development of antidiabetic drugs. Medicinally privileged triazole structures, specifically 1,2,3-triazol and 1,2,4-triazoles, fused with other heterocyclic rings, have shown promising antidiabetic activity. This review summarizes the structure-activity relationship, enzyme inhibitory activity, and patents filed of these scaffolds as alpha-amylase and alpha-glucosidase inhibitors.