:
Selective GluN2B/N-methyl-D-aspartate receptor (NMDAR) antagonists have exposed their clinical effectiveness in cluster of neurodegenerative diseases such as Epilepsy, Alzheimer’s disease, Parkinson’s disease, pain and depression. Hence, GluN2B/NMDAR is considered to be a prospective target for the management of neurodegenerative diseases. Here, we have discussed current results and significance of subunit selective GluN2B/NMDAR antagonists to pave the way for establishment of new, safe, and economical drug candidate in a near future. Using summarized data of selective GluN2B/NMDAR antagonists, medicinal chemists become certainly a step closer to a goal of improving therapeutic and side effect profile of selective antagonists. Outlined summary of designing strategies, synthetic schemes, and pharmacological evaluation studies reinvigorate efforts to identify, modify, and synthesize novel GluN2B/NMDAR antagonists to treat neurodegenerative diseases.
Background:
Diabetes mellitus (DM) is the most severe, chronic metabolic disorder with abnormally elevated
concentration of plasma glucose levels, leading to significant complications, such as diabetic neuropathy, retinopathy, and
cardiovascular illnesses.
Objective:
Synthetic drugs have some disadvantages and limitations. Therefore, there is a continuous global and insisting
need for new and better treatment options for the Diabetes Mellitus.
Method:
In this study, 42 natural antidiabetic constituents like alkaloids, glycosides and flavonoids were selected on the basis
of mechanism of action on various molecular targets such as, Glucokinase activator, Dipeptidyl peptidase 4 (DPP-4), peroxisome
proliferator-activated receptors (PPARγ), and α-glucosidase inhibitor. To investigate the potential molecular targets
for natural antidiabetcs agents molecular docking study was carried out using Glide module of Schrodinger Suit.
Results and Discussion:
Interactions of specific amino acid of the targets with the atoms of the chemical constituents and
their Gscore indicate the proper binding of the chemical constituents with target. The results revealed that Myricetin, Quercetin
are interactiing with active sites of the target chosen and can be used for the designing of novel compounds as antidibetics.
Conclusion:
Calculated GScore could be used as a preliminary tool for screening of antidiabetic drugs before performing
experimental activity.
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