Recent Developments in the Synthesis of N‐Heterocyclic Compounds as α‐Amylase Inhibitors via In‐Vitro and In‐Silico Analysis: Future Drugs for Treating Diabetes

Abstract

In nature, N‐heterocyclic compounds and their derivatives are abundant. They serve as the building blocks of many biological entities, such as enzymes, alkaloids, hormones, antibiotics, and vitamins. The treatment of diabetes is one of the major applications of heterocyclic compounds. Natural as well as synthetic, both types of heterocyclic compounds show anti‐diabetic activity. There is a plethora of literature on the hyper/hypoglycaemic activity of natural compounds. This review discusses the synthesis methods, yields of the reactions and Inhibitory concentration (IC50) values of all the synthesized derivatives via different assays such as 3,5‐dinitrosalicylic acid (DNS) or starch assays. IC50 values of all the derivatives have been compared with those of standard acarbose. Structure activity relationship of most potential compounds with α‐amylase enzyme is established to show the type of interactions between them. Molecular docking studies show the type of interaction between compounds and enzyme.

Synthesis of Pyrazoline‐Embedded 1,2,3‐Triazole Derivatives via 1,3‐Dipolar Cycloaddition Reactions with in vitro and in silico Studies

“…Synthetic routes for the synthesis of 1,2,3 triazole hybrids by the click chemistry method have been reported [26–29] . But, few reports of pyrazoline bearing 1,2,3 triazole derivatives showing α‐glycosidase and α‐amylase activity are found in literature [30–36] . Inspired by this, we have synthesized pyrazoline bearing 1,2,3‐triazole and they were subjected for α‐glycosidase and α‐amylase inhibitory and antioxidant activity.…”

“…[26][27][28][29] But, few reports of pyrazoline bearing 1,2,3 triazole derivatives showing α-glycosidase and α-amylase activity are found in literature. [30][31][32][33][34][35][36] Inspired by this, we have synthesized pyrazoline bearing 1,2,3-triazole and they were subjected for α-glycosidase and α-amylase inhibitory and antioxidant activity. Further, we have also carried out the in silico studies for the synthesized compounds through molecular docking and simulation.…”

Dicationic copper(i) complexes bearing ENE (E = S, Se) pincer ligands; catalytic applications in regioselective cyclization of 1,6-diynes

“…Oxazole heterocycles are an important class of structural motifs found in numerous natural products and pharmacologically active synthetic drug molecules due to their biological activities. 1 A vast variety of synthetic protocols have been developed for the construction of differently substituted oxazole derivatives through metal-mediated and metal-free catalytic approaches 2 by using different substrates. Click chemistry is one of the widely employed techniques for the synthesis of oxazoles and triazoles.…”

Optimisation of alpha-amylase inhibitor production in solid state fermentation

“…Related research has involved purification and the elucidation of characteristics, application and clinical trials, expression of gene in competent microorganisms, uses as nutraceutical agent among others, including a more recent publication on the incorporation of P. vulgaris in yoghurt for the control of blood glucose in hyperglycemic mice via the modulation of microorganisms in the gastrointestinal tract ( Wang et al, 2021 ). While numerous plant sources exist and have been identified, synthetic types including miglitol, acarbose, voglibose and indazoles also exist ( DiNicolantonio et al, 2015 ; Garg et al, 2022 ). Submerged fermentation of filamentous bacteria of the genus Streptomyces has also yielded alpha-amylase inhibitors which have been variously characterized and applied ( Manivasagan et al, 2015 ).…”