Solvent-free synthesis, biological evaluation and in silico studies of novel 2-amino-7-(bis(2-hydroxyethyl)amino)-4H-chromene-3-carbonitrile derivatives as potential a-amylase inhibitors

Chothani, Savankumar R.; Dholariya, Monil P.; Joshi, Rupal J.; Chamakiya, Chirag A.; Maliwal, Deepika; Pissurlenkar, Raghuvir R.S.; Patel, Anilkumar S.; Bhalodia, Jasmin J.; Ambasana, Mrunal A.; Patel, Rashmiben B.; Bapodra, Atul H.; Kapuriya, Naval P.

doi:10.1016/j.molstruc.2023.137462

Journal of Molecular Structure

2024

DOI: 10.1016/j.molstruc.2023.137462

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Solvent-free synthesis, biological evaluation and in silico studies of novel 2-amino-7-(bis(2-hydroxyethyl)amino)-4H-chromene-3-carbonitrile derivatives as potential a-amylase inhibitors

Savankumar R. Chothani,

Monil P. Dholariya,

Rupal J. Joshi

et al.

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2024

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Cited by 2 publications

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Synthesis, antidiabetic activity and in silico studies of benzo[b]thiophene based small molecule α-amylase inhibitors

Joshi,

Dholariya,

Chothani

et al. 2024

Journal of Molecular Structure

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Synthesis, antidiabetic activity and in silico studies of benzo[b]thiophene based small molecule α-amylase inhibitors

Joshi,

Dholariya,

Chothani

et al. 2024

Journal of Molecular Structure

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Indole–thiazolidinedione–triazole hybrids: synthesis, molecular docking, absorption, distribution, metabolism and excretion (ADME) profiling, and biological evaluation as α-amylase inhibitors

Dholariya,

Patel

2024

Chemistry Letters

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A novel series of hybrid indole–thiazolidinedione–triazole derivatives (6a-l) were synthesized and assessed for their in vitro inhibitory activity against porcine pancreatic α-amylase. The synthetic procedure consists of 3 steps. A crucial step in this process involves the generation of novel target molecules using a Cu(I)-catalyzed azide–alkyne cycloaddition reaction. The α-amylase inhibition IC50 value of the targeted compounds ranged from 0.51 ± 0.02 to 7.99 ± 0.28 μM as compared with 0.68 ± 0.02 μM with acarbose as the standard drug. Using the Autodock technique, all the derivatives 6a-l were subjected to molecular docking investigations against porcine pancreatic α-amylase (PDB ID: 1OSE). Moreover, it was discovered that the docked compounds had excellent binding affinities that ranged from −10.1 to −10.8 kcal/mol as compared with the standard −7.9 kcal/mol. Additionally, a comprehensive analysis of the physicochemical and pharmacokinetic properties associated with absorption, distribution, metabolism and excretion (ADME) was conducted for all the synthesized compounds.

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Solvent-free synthesis, biological evaluation and in silico studies of novel 2-amino-7-(bis(2-hydroxyethyl)amino)-4H-chromene-3-carbonitrile derivatives as potential a-amylase inhibitors

Cited by 2 publications

References 51 publications

Synthesis, antidiabetic activity and in silico studies of benzo[b]thiophene based small molecule α-amylase inhibitors

Synthesis, antidiabetic activity and in silico studies of benzo[b]thiophene based small molecule α-amylase inhibitors

Indole–thiazolidinedione–triazole hybrids: synthesis, molecular docking, absorption, distribution, metabolism and excretion (ADME) profiling, and biological evaluation as α-amylase inhibitors

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