ArticleMolecules (Basel, Switzerland)2022
New Biologically Hybrid Pharmacophore Thiazolidinone-Based Indole Derivatives: Synthesis, In Vitro Αlpha-Amylase and Αlpha-Glucosidase Along with Molecular Docking Investigations.
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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11 citing papers in PubMed, 31 citations in OpenAlex.
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- Fused Imidazotriazole-Based Therapeutics: A Multidisciplinary Study Against Diabetes-Linked Enzymes Alpha-Amylase and Alpha-Glucosidase Using In Vitro and In Silico Methods.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Development of Novel α-Amylase Inhibitors: Synthesis, Molecular Docking, and Biochemical Studies.Cell biochemistry and biophysics · 2025Article
- In-silico analysis of potential phytochemicals targeting mitogen activating protein kinase-14 (MAPK14) gene in colorectal cancer.Scientific reports · 2025Article
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- Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis,RSC medicinal chemistry · 2024Article
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- Novel indole based fused triazole-thiadiazole derivatives as anti-diabetic agents:Future medicinal chemistry · 2024Article
- Imidazopyridine-Based Thiazole Derivatives as Potential Antidiabetic Agents: Synthesis, In Vitro Bioactivity, and In Silico Molecular Modeling Approach.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Blood indices of omega-3 and omega-6 polyunsaturated fatty acids are altered in hyperglycemia.Saudi journal of biological sciences · 2023Article
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Authors and funding
13 authors at 7 institutions in 2 countries.
Funding
Abstract
Amylase and glucosidase enzymes are the primary harmful source in the development of the chronic condition known as diabetes mellitus. The main function of these enzymes is to break the macromolecules into simple sugar units which are directly involved in the solubility of blood, hence increasing blood glucose levels. To overcome this effect, there is a need for a potent and effective inhibitor that inhibits the conversion of macromolecules of sugar into its smaller units. In this regard, we synthesized thiazolidinone-based indole derivatives (1−20). The synthesized derivatives were evaluated for α-amylase and α-glucosidase inhibitory activity. Different substituted derivatives were found with moderate to good potentials having IC50 values ranging, for α-amylase, from 1.50 ± 0.05 to 29.60 ± 0.40 μM and, for α-glucosidase, from IC50 = 2.40 ± 0.10 to 31.50 ± 0.50 μM. Among the varied substituted compounds, the most active analogs four (1.80 ± 0.70 and 2.70 ± 0.70), five (1.50 ± 0.05 and 2.40 ± 0.10, respectively) of the series showed few folds better inhibitory activity than standard drug acarbose (IC50 = 10.20 ± 0.10 and 11.70 ± 0.10 μM, respectively). Moreover, structure−activity relationship (SAR) was established and binding interactions were analyzed for ligands and proteins (α-amylase and α-glucosidase) through a molecular docking study.
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