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 4 publications

References 51 publications

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2‐Chloroquinolinyl‐thiazolidine‐2,4‐dione Hybrids as Potential α‐Amylase Inhibitors: Synthesis, Biological Evaluations, and In Silico Studies

Karmur,

Dholariya,

Patel

et al. 2024

ChemistrySelect

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Recently, molecular hybridization strategy has paved a way to develop novel lead compounds for the α‐amylase targeted antidiabetic therapy. In this study, we disclosed a series of new hybrids of thiazolidine‐2,4‐diones with 2‐chloroquinoline‐3‐yl moiety as potential antidiabetic agents. The molecular structures of all the synthesized hybrids (15a–n) were confirmed by spectroscopic studies (FT‐IR, ESI‐MS, 1H, 13C NMR, and elemental analysis). When in vitro antidiabetic evaluation of these agents was carried out in a dose‐dependent manner, it was revealed that several compounds (15f–h, 15j, and 15n) were endowed with significant antidiabetic activities and exhibited more than 50% α‐amylase inhibition at a dose of 50 µg/mL. Particularly, hybrid 15n was found to be more potent than acarbose with 95% inhibition of α‐amylase and IC50 of 5.00 ± 0.18 µM under given conditions. Further, it was demonstrated that 15n bearing 2‐chloroquinolinyl and thiazolidin‐2,4‐dione scaffolds functionalized with 3‐OMe and 4‐OH groups was not only able to effectively bind with α‐amylase receptor site with best docking score (−9.644 kcal/mol) but also possessed drug‐likenesses properties with no violations of Lipinski rule. Overall, this study discovered new 2‐chloroquinolinyl‐thiazolidine‐2,4‐diones hybrids as novel α‐amylase inhibitors and compound 15n as promising lead for its further development as antidiabetic agent.

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2‐Chloroquinolinyl‐thiazolidine‐2,4‐dione Hybrids as Potential α‐Amylase Inhibitors: Synthesis, Biological Evaluations, and In Silico Studies

Karmur,

Dholariya,

Patel

et al. 2024

ChemistrySelect

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Efficient one-pot tandem C-C formation reaction catalyzed by a multi-functionalized polyacrylonitrile fiber catalyst

Li,

Cui,

Chen

et al. 2024

Journal of Environmental Chemical Engineering

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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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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 4 publications

References 51 publications

2‐Chloroquinolinyl‐thiazolidine‐2,4‐dione Hybrids as Potential α‐Amylase Inhibitors: Synthesis, Biological Evaluations, and In Silico Studies

2‐Chloroquinolinyl‐thiazolidine‐2,4‐dione Hybrids as Potential α‐Amylase Inhibitors: Synthesis, Biological Evaluations, and In Silico Studies

Efficient one-pot tandem C-C formation reaction catalyzed by a multi-functionalized polyacrylonitrile fiber catalyst

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

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