This study was carried out to synthesize benzotriazole-based bis-Schiff base scaffolds (1–20) and assess them in vitro for α-glucosidase inhibitory potentials. All the synthetics analogs based on benzotriazole-based bis-Schiff base scaffolds were found to display an outstanding inhibition profile on screening against the α-glucosidase enzyme. The synthetic scaffolds showed a varied range of inhibition profiles having IC50 values ranging from 1.10 ± 0.05 µM to 28.30 ± 0.60 µM when compared to acarbose as a standard drug (IC50 = 10.30 ± 0.20 µM). Among the series, fifteen scaffolds 1–3, 5, 6, 9–16, 18–20 were identified to be more potent than standard acarbose, while the five remaining scaffolds 4, 7, 8, 16, and 17, also showed potency against the α-glucosidase enzyme but were found to be less potent than standard acarbose. The structure of all the newly synthesized scaffolds was confirmed using different spectroscopic techniques such as HREI-MS and 1H- and 13C- NMR spectroscopy. To find a structure-activity relationship, molecular docking studies were carried out to understand the binding mode of the active inhibitors with the active sites of the enzyme and the results supported the experimental data.
There is an increasing prevalence of diabetes mellitus
throughout
the world, and new compounds are necessary to combat this. The currently
available antidiabetic therapies are long-term complicated and side
effect-prone, and this has led to a demand for more affordable and
more effective methods of tackling diabetes. Research is focused on
finding alternative medicinal remedies with significant antidiabetic
efficacy as well as low adverse effects. In this research work, we
have focused our efforts to synthesize a series of 1,2,4-triazole-based
bis-hydrazones and evaluated their antidiabetic properties. In addition,
the precise structures of the synthesized derivatives were confirmed
with the help of various spectroscopic techniques including 1H-NMR, 13C-NMR, and HREI-MS. To find the antidiabetic
potentials of the synthesized compounds, in vitro α-glucosidase
and α-amylase inhibitory activities were characterized using
acarbose as the reference standard. From structure–activity
(SAR) analysis, it was confirmed that any variation found in inhibitory
activities of both α-amylase and α-glucosidase enzymes
was due to the different substitution patterns of the substituent(s)
at variable positions of both aryl rings A and B. The results of the
antidiabetic assay were very encouraging and showed moderate to good
inhibitory potentials with IC50 values ranging from 0.70
± 0.05 to 35.70 ± 0.80 μM (α-amylase) and 1.10
± 0.05 to 30.40 ± 0.70 μM (α-glucosidase). The
obtained results were compared to those of the standard acarbose drug
(IC50 = 10.30 ± 0.20 μM for α-amylase
and IC50 = 9.80 ± 0.20 μM for α-glucosidase).
Specifically, compounds 17, 15, and 16 were found to be significantly active with IC50 values of 0.70 ± 0.05, 1.80 ± 0.10, and 2.10 ± 0.10
μM against α-amylase and 1.10 ± 0.05, 1.50 ±
0.05, and 1.70 ± 0.10 μM against α-glucosidase, respectively.
These findings reveal that triazole-containing bis-hydrazones act
as α-amylase and α-glucosidase inhibitors, which help
develop novel therapeutics for treating type-II diabetes mellitus
and can act as lead molecules in drug discovery as potential antidiabetic
agents.
The goal of this study is to determine the link between educational and religious freedom and prosperity in 45 countries from 2009 to 2018. Using the GMM system, the researchers were able to analyze the data. They found that academic and religious freedom is associated with increased prosperity. The collaboration of religious and academic freedom is also positive, which indicates that the two factors can contribute to the increase in prosperity. The researchers introduced the term "government effectiveness" to describe the relationship between capital formation and economic prosperity. The researchers used trade openness and gross fixed capital formation as control variables. Although they have a positive impact on the overall economy, they are not able to provide a significant boost to the prosperity of low-income countries. Therefore, the researchers recommend that educational and religious freedom be included in the government's efforts to improve the economic prosperity of these countries.
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