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Journal articles on the topic 'Derivatives of alpha-glucosidase inhibitors'

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Published: 5 June 2025

Last updated: 2 August 2025

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1

Nursamsiar, Nursamsiar, Marwati Marwati, Khairuddin Khairuddin, et al. "Isolation, characterization, and in vitro inhibitory activity of a new alpha-glucosidase inhibitor from Schleichera oleosa (Lour.) Oken leaves." Journal of Pharmacy & Pharmacognosy Research 13, no. 1 (2025): 140–51. http://dx.doi.org/10.56499/jppres24.1960_13.1.140.

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Context: The development of novel and potent alpha-glucosidase inhibitors from natural sources holds immense promise for treating diabetes. Aims: To identify the isolated compound, determine its inhibitory potency, explore its molecular interactions with the alpha-glucosidase receptor, and understand the role of specific structural features in its inhibitory activity. Methods: Research began with the isolation and identification of the new gallic acid derivative of the Schleichera oleosa leaf extract. The isolated compound (1) was characterized as 3,5-dihydroxy-4-methoxybenzoic acid using spec

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2

Field, R. A., A. H. Haines, E. J. T. Chrystal, and M. C. Luszniak. "Histidines, histamines and imidazoles as glycosidase inhibitors." Biochemical Journal 274, no. 3 (1991): 885–89. http://dx.doi.org/10.1042/bj2740885.

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This present study reports the ability of a range of derivatives of L-histidine, histamine and imidazole to act as inhibitors of sweet-almond β-glucosidase, yeast alpha-glucosidase and Escherichia coli β-galactosidase. The addition of a hydrophobic group to the basic imidazole nucleus greatly enhances binding to both the alpha- and β-glucosidases. L-Histidine (beta-naphthylamide (Ki 17 microM) is a potent competitive inhibitor of sweet-almond β-glucosidase as is omega-N-acetylhistamine (K1 35 microM), which inhibits the sweet-almond β-glucosidase at least 700 times more strongly than either ye

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3

Ankireddy, Ashok Reddy, Rambabu Gundla, Tuniki Balaraju, et al. "Quinazolin derivatives as emerging alpha-glucosidase inhibitors." European Journal of Chemistry 9, no. 4 (2018): 322–30. http://dx.doi.org/10.5155/eurjchem.9.4.322-330.1748.

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A series of C-7 substituted-2-morpholino-N-(pyridin-2-ylmethyl)quinazolin-4-amine have been synthesized and biochemical assay was examined against α-glucosidase function inhibition activity. A structure activity and structure property relationship study was experimented to surface the new hit compound. This study led to the identification of C-7substituted quinazolines with minimum inhibitory concentrations (MICs) in the preffered micromolar range in addition with interesting physicochemical properties. Biological evaluation yielded eight analogs which rose with significant α-glucosidase inhib

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4

K, Gupta. "3D-QSAR Analysis and Molecular Docking Studies on 3-Arylcoumarin Derivatives as Potential α- Glucosidase Inhibitors". Medicinal Chemistry 10, № 6 (2020): 5. https://doi.org/10.5281/zenodo.10669459.

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α-glucosidase inhibitors (AGI) are the structural moieties that are found to be of utmost importance in the fields of pharmacy and which involves delaying the absorption of carbohydrates by blocking of alpha-glucosidase enzyme in the brush border of small intestine and plays an important role in constituting a promising therapeutic class against diabetic disease (Type II). In this study, the three-dimensional quantitative structure-activity relationship (3D-QSAR) and docking models were developed using Fujito-Ban analysis in VALSTAT software and Molegro Virtual Docker 6.0. The theoretica

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5

M, Heravi; Majid, M. Mohammadi-Khanaposhtani, H. Yahyavi та ін. "New Biscoumarin Derivatives as Potent α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study". Polycyclic Aromatic Compounds 40, № 7 (2020): 915–26. https://doi.org/10.1080/10406638.2018.1509359.

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A new series of biscoumarin derivatives 3a–n were synthesized and evaluated for their α-glucosidase inhibitory activities. The reaction of the 4-aminocoumarin with benzaldehyde derivatives led to the formation of the title compounds in good yields. All the synthesized compounds showed potent α-glucosidase inhibitory activity with IC<sub>50</sub> ranging from 20.0 ± 0.7 to180.1 ± 0.8 µM, in comparison with acarbose as the standard drug (IC<sub>50</sub> = 750.0 1.5 µM). Among the synthesized compounds, 3,3'-(p-tolylmethylene)bis(4-am

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6

Bule, Mohammed Hussen, Roghaieh Esfandyari, Tadesse Bekele Tafesse, Mohsen Amini, Mohammad Ali Faramarzi та Mohammad Abdollahi. "Synthesis, Molecular Docking and α-Glucosidase Inhibitory Activity Study of 2,4,6-triaryl Pyrimidine Derivatives". Letters in Drug Design & Discovery 17, № 10 (2020): 1216–26. http://dx.doi.org/10.2174/1570180817666200103130536.

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Background: α-Glucosidase inhibitors hinder the carbohydrate digestion and play an important role in the treatment of diabetes mellitus. α-glucosidase inhibitors available on the market are acarbose, miglitol, and voglibose. However, the use of acarbose is diminishing due to related side effects like diarrhea, bloating and abdominal distension. Objectives: This study aimed to synthesize 2,4,6-triaryl pyrimidines derivatives, screen their α- glucosidase inhibitory activity, perform kinetic and molecular docking studies. Methods: A series of 2,4,6-triaryl pyrimidine derivatives were synthesized

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7

Abchir, Oussama, Meriem Khedraoui, Imane Yamari, et al. "Exploration of alpha-glucosidase inhibitors: A comprehensive in silico approach targeting a large set of triazole derivatives." PLOS ONE 19, no. 9 (2024): e0308308. http://dx.doi.org/10.1371/journal.pone.0308308.

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Background The increasing prevalence of diabetes and the side effects associated with current medications necessitate the development of novel candidate drugs targeting alpha-glucosidase as a potential treatment option. Methods This study employed computer-aided drug design techniques to identify potential alpha-glucosidase inhibitors from the PubChem database. Molecular docking was used to evaluate 81,197 compounds, narrowing the set for further analysis and providing insights into ligand-target interactions. An ADMET study assessed the pharmacokinetic properties of these compounds, including

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8

Ernawati, Teni, Maksum Radji, Muhammad Hanafi, Abdul Mun’im та Arry Yanuar. "Cinnamic Acid Derivatives as α-Glucosidase Inhibitor Agents". Indonesian Journal of Chemistry 17, № 1 (2017): 151. http://dx.doi.org/10.22146/ijc.23572.

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This paper reviews biological activity of some cinnamic acid derivative compounds which are isolated from natural materials and synthesized from the chemical compounds as an agent of α-glucosidase inhibitors for the antidiabetic drug. Aegeline, anhydroaegeline and aeglinoside B are natural products isolated compounds that have potential as an α-glucosidase inhibitor. Meanwhile, α-glucosidase inhibitor class of derivatives of cinnamic acid synthesized compounds are p-methoxy cinnamic acid and p-methoxyethyl cinnamate. Chemically, cinnamic acid has three main functional groups: first is the subs

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9

Hernández, Brandón, María del Carmen Cruz, Omar Gómez, Elvia Becerra, Fabiola Eloisa Jiménez, and Aaron Mendieta. "Alpha-glucosidase and Alpha-amylase Inhibitors Derived from Naturally Occurring Prenylated Isoflavones." Journal of the Mexican Chemical Society 68, no. 1 (2024): 156–69. http://dx.doi.org/10.29356/jmcs.v68i1.2129.

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A series of prenylated isoflavones were synthesized to evaluate their inhibitory effect against α-glucosidase and α-amylase enzymes, analyzing the bioisosteric effect of the linear or cyclized prenyl moiety in these benzopyran derivatives. Compound 5a exhibited higher α-glucosidase inhibition (IC50 = 60.5 µM) and lower α-amylase inhibition (IC50 = 85.0 µM) compared to acarbose (IC50 = 527.5 µM for α-glucosidase and 20.1 µM for α-amylase). In contrast, prenylated isoflavone 5c showed higher inhibition in both enzymes (IC50 = 17.6 µM for α-glucosidase and 21.2 µM for α-amylase). This suggests th

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10

Ullah, Saeed, Salma Mirza, Uzma Salar, et al. "2-Mercapto Benzothiazole Derivatives: As Potential Leads for the Diabetic Management." Medicinal Chemistry 16, no. 6 (2020): 826–40. http://dx.doi.org/10.2174/1573406415666190612153150.

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Background: Results of our previous studies on antiglycation activity, and the noncytotoxicity of 2-mercapto benzothiazoles, encouraged us to further widen our investigation towards the identification of leads against diabetes mellitus. Methods: 33 derivatives of 2-mercapto benzothiazoles 1-33 were evaluated for in vitro α- glucosidase inhibitory activity. Mode of inhibition was deduced by kinetic studies. To predict the interactions of 2-mercapto benzothiazole derivatives 1-33 with the binding pocket of α-glucosidase enzyme, molecular docking studies were performed on the selected inhibitors.

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11

Li, Mengyue, Lin Li, Li Lu, Xuetao Xu, Jinhui Hu та Jin-Bao Peng. "Anti-α-Glucosidase, SAR Analysis, and Mechanism Investigation of Indolo[1,2-b]isoquinoline Derivatives". Molecules 28, № 13 (2023): 5282. http://dx.doi.org/10.3390/molecules28135282.

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To find potential α-glucosidase inhibitors, indolo[1,2-b]isoquinoline derivatives (1–20) were screened for their α-glucosidase inhibitory effects. All derivatives presented potential α-glucosidase inhibitory effects with IC50 values of 3.44 ± 0.36~41.24 ± 0.26 μM compared to the positive control acarbose (IC50 value: 640.57 ± 5.13 μM). In particular, compound 11 displayed the strongest anti-α-glucosidase activity, being ~186 times stronger than acarbose. Kinetic studies found that compounds 9, 11, 13, 18, and 19 were all reversible mix-type inhibitors. The 3D fluorescence spectra and CD spectr

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12

Chochkova, Maya G., Petranka P. Petrova, Boyka M. Stoykova та ін. "Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition". Journal of Chemistry 2017 (2017): 1–5. http://dx.doi.org/10.1155/2017/6080129.

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Currently, there is an increasing interest towardsα-glucosidase inhibition of various diseases including diabetes mellitus type 2, cancer, HIV, and B- and C-type viral hepatitis. Cinnamic acid derivatives have been shown to be potentially valuable as a new group ofα-glucosidase inhibitors. Therefore, herein, theα-glucosidase inhibitory activity oftrans-N-cinnamoyl and hydroxycinnamoyl amides was studied in vitro. Results revealed that the tested hydroxycinnamoyl amides (1–16) inhibiteda-glucosidase with IC50s ranging between 0.76 and 355.1 μg/ml. Compounds1,2,5,6,9,14, and15showed significant

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13

Bashir, Muhammad A., Kulsoom Javaid, Muniza Shaikh, Muhammad I. Choudhary та Hina Siddiqui. "Tyramine Derivatives as Potent Therapeutics for Type 2 Diabetes: Synthesis and In Vitro Inhibition of α-Glucosidase Enzyme". Medicinal Chemistry 16, № 8 (2020): 1124–35. http://dx.doi.org/10.2174/1573406416666200128114422.

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Background: Tyramine derivatives 3-16 were prepared and tested first time for their α- glucosidase (Sources: Saccharomyces cerevisiae) inhibitory activity by using an in vitro mechanismbased biochemical assay. All the compounds were found to be new, except compounds 3, 10-12 and 16. Objective: In continuation of our research to synthesize and identify potent inhibitors of α-glucosidase enzyme, we intended to synthesize new inhibitors of α-glucosidase enzyme with enhanced efficacy in order to provide the basis for the better treatment of the type-II diabetic. Methods: Tyramine (1) was allowed t

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14

Patil, Shashank M., Reshma Mary Martiz, A. M. Satish та ін. "Discovery of Novel Coumarin Derivatives as Potential Dual Inhibitors against α-Glucosidase and α-Amylase for the Management of Post-Prandial Hyperglycemia via Molecular Modelling Approaches". Molecules 27, № 12 (2022): 3888. http://dx.doi.org/10.3390/molecules27123888.

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Coumarin derivatives are proven for their therapeutic uses in several human diseases and disorders such as inflammation, neurodegenerative disorders, cancer, fertility, and microbial infections. Coumarin derivatives and coumarin-based scaffolds gained renewed attention for treating diabetes mellitus. The current decade witnessed the inhibiting potential of coumarin derivatives and coumarin-based scaffolds against α-glucosidase and α-amylase for the management of postprandial hyperglycemia. Hyperglycemia is a condition where an excessive amount of glucose circulates in the bloodstream. It occur

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15

Bui, Thanh Q., Bui Thi Thoi, Phan Tu Quy, et al. "In silico screening for inhibitory potentiality towards protein structure tyrosine phosphatase 1B of sulfonylureas derivatives." Vietnam Journal of Chemistry 60, no. 1 (2022): 123–32. http://dx.doi.org/10.1002/vjch.202100120.

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AbstractSulfonylureas derivatives were demonstrated to be effective inhibitors towards α‐glucosidase, thus also expected possessing inhibitory potentiality towards tyrosine phosphatase structure 1B. Five new sulfonylureas derivatives (S1‐S5), exhibiting α‐glucosidase inhibition activity, were selected for in silico screening for inhibitability towards UniProtKB‐PTP1B structure. Density functional theory confirms their existence; natural bond orbital analysis infers their stability; electronic transferability suggests their capability regarding intermolecular interaction. Docking‐based investig

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16

Şenkardeş, Sevil, та Zeynep Hanne Baş. "Synthesis, Structural Elucidation and α-Glucosidase Inhibitory Activity of New Hydrazide Derivatives". Yüzüncü Yıl Üniversitesi Fen Bilimleri Enstitüsü Dergisi 30, № 1 (2025): 69–77. https://doi.org/10.53433/yyufbed.1613136.

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Diabetes mellitus (DM) is a chronic and progressive metabolic disorder affecting over 422 million people globally. It arises from insufficient insulin production or the inability of cells to respond to insulin, leading to disruptions in carbohydrate, fat, and protein metabolism. Over time, DM can result in severe complications such as cardiovascular diseases, kidney failure, and vision loss. Effective management of DM includes therapeutic strategies aimed at stabilizing blood glucose levels. Among these, α-glucosidase enzyme inhibitors play a crucial role by slowing carbohydrate digestion and

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17

Ali, Majid, Khuram Malik, Asma Zaidi та ін. "In-vitro high-throughput library screening—Kinetics and molecular docking studies of potent inhibitors of α-glucosidase". PLOS ONE 18, № 6 (2023): e0286159. http://dx.doi.org/10.1371/journal.pone.0286159.

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High throughput screening of synthetic compounds against vital enzymes is the way forward for the determination of potent enzyme inhibitors. In-vitro high throughput library screening of 258 synthetic compounds (comp. 1–258), was performed against α-glucosidase. The active compounds out of this library were investigated for their mode of inhibition and binding affinities towards α-glucosidase through kinetics as well as molecular docking studies. Out of all the compounds selected for this study, 63 compounds were found active within the IC50 range of 3.2 μM to 50.0 μM. The most potent inhibito

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18

Talab, Faiz, Zainab, Aftab Alam, et al. "Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches." Future Medicinal Chemistry 15, no. 23 (2023): 2195–208. http://dx.doi.org/10.4155/fmc-2023-0232.

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Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of α-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Methods: Polyhydroquinoline derivatives (1–17) were synthesized and tested for in vitro α-glucosidase inhibitory activity. Results: All the synthesized compounds exhibited excellent to good inhibitory activity, having IC50 values from 1.23 ± 0.03 to 73.85 ± 0.61 μM, compared with the standard drug, acarbose. The binding mechanism of these derivatives with

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19

Asnawi, Aiyi, Shifa Mieldianisa, Widhya Aligita, Anne Yuliantini, and Ellin Febrina. "Integrative computational approaches for designing novel alpha-glucosidase inhibitors based on curculigoside A derivatives: Virtual screening, molecular docking, and molecular dynamics." Journal of Herbmed Pharmacology 13, no. 2 (2024): 308–23. http://dx.doi.org/10.34172/jhp.2024.49407.

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Introduction: Over 422 million people worldwide suffer from diabetes, causing 1.5 million fatalities annually. The existing medications have shortcomings, including poor glucose control and adverse effects. The present study aimed to create possible alpha-glucosidase inhibitors utilizing a curculigoside A derivative ligand-based model. Methods: A pharmacophore model was constructed utilizing the structure information of curculigoside A derivatives and PharmaGist. Subsequently, virtual screening, molecular docking, and molecular dynamics were employed to simulate the hits. Results: From six tra

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20

Sasikala, M., S. Mohan, M. Geetha, E. Nisha, N. Narmadha, and A. Nagarajan. "In silico design, synthesis and characterization of quercetin derivatives as anti-diabetic agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 04 (2024): 513. https://doi.org/10.59467/ijhc.2024.34.513.

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Diabetes mellitus is a dominant metabolic condition noticeable by determined high blood sugar levels, stanching from either poor insulin production or insulin resistance. Managing diabetes often includes hindering enzymes, such as alpha-amylase and alpha-glucosidase to control blood glucose points after meals. Natural polyphenols, such as quercetin, have proved major enzyme inhibitory activity, leading to developing interest in reviewing quercetin derivatives as prospective antidiabetic agents. This research emphasizes on the design, synthesis, and assessment of quercetin ester derivatives for

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21

Khalid, Zunera, Maha Abdallah Alnuwaiser, Hafiz Adnan Ahmad, et al. "Experimental and Computational Analysis of Newly Synthesized Benzotriazinone Sulfonamides as Alpha-Glucosidase Inhibitors." Molecules 27, no. 20 (2022): 6783. http://dx.doi.org/10.3390/molecules27206783.

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Diabetes mellitus is a chronic metabolic disorder in which the pancreas secretes insulin but the body cells do not recognize it. As a result, carbohydrate metabolism causes hyperglycemia, which may be fatal for various organs. This disease is increasing day by day and it is prevalent among people of all ages, including young adults and children. Acarbose and miglitol are famous alpha-glucosidase inhibitors but they complicate patients with the problems of flatulence, pain, bloating, diarrhea, and loss of appetite. To overcome these challenges, it is crucial to discover new anti-diabetic drugs

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Khaldan, Ayoub, Soukaina Bouamrane, Reda El-Mernissi та ін. "Integrated computer aided methods to designing potent α-Glucosidase inhibitors based on quinoline scaffold derivative". Current Chemistry Letters 14, № 1 (2025): 79–106. http://dx.doi.org/10.5267/j.ccl.2024.9.003.

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Diabetes mellitus is a serious health disease that affects people all over the world. The number of persons identified with diabetes mellitus rises each year. α -Glucosidase is a digestive enzyme used to control diabetes mellitus. The searching for new potent α-glucosidase inhibitors capable of delaying carbohydrate digestion in the human body is an important strategy towards control of diabetes mellitus. In this work, a series of quinoline-based Schiff base derivatives already identified as α-glucosidase inhibitory activity was studied by using 2D/3D-QSAR approach. The best HQSAR/A-B-C-H-Ch-D

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23

Gungor, Ozge, Seda Nur Kertmen Kurtar та Muhammet Kose. "Water soluble biguanide salts and their 1,3,5-triazine derivatives as inhibitors of acetylcholinesterase and α-glucosidase". Zeitschrift für Kristallographie - Crystalline Materials 235, № 10 (2020): 465–75. http://dx.doi.org/10.1515/zkri-2020-0025.

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AbstractSeven biguanide derivatives were prepared by the nucleophilic reaction between dicyandiamide and p-substitute aniline derivatives or memantine or adamantine under acidic conditions. The cyclization of the biguanide compounds were also conducted via acetone to give 1,3,5-triazine derivatives. The structures of the synthesized compounds were characterized by analytical methods. The solid state structures of [HL5]Cl, [H2L7]Cl2, [HL1a]Cl and [HL5a]Cl were investigated by X-ray diffraction study. The acetylcholinesterase and α-glucosidase inhibitor properties of the compounds were then eval

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24

Wang, Yu-ling, Ting-jian Zhang, Jing-wei Liang, Fan-hao Meng та Shao-jie Wang. "Synthesis and Biological Evaluation of New Substituted 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one Derivatives asα-Glucosidase Inhibitors". Journal of Chemistry 2014 (2014): 1–6. http://dx.doi.org/10.1155/2014/590129.

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A series of new substituted 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives bearing groups methoxy,tert-butyl, and atoms of halogens at thepara-position of the A-ring were synthesized andin vitrobiological activities were evaluated as nonsugarα-glucosidase inhibitors. Most of the test compounds demonstrated significantα-glucosidase inhibitory activity relative to that of Acarbose (IC50= 29.26 μM). Thepara-substitution with a methoxy group or halogens could notably increase the potency. Compounds17,18, and23, with IC50values of 0.025 μM, 0.014 μM, and 0.018 μM, respectively,

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Wang, Jiangming, Silei Lu, Ruilong Sheng, Junting Fan, Wenhui Wu та Ruihua Guo. "Structure-Activity Relationships of Natural and Synthetic Indole-Derived Scaffolds as α-Glucosidase Inhibitors: A Mini-Review". Mini-Reviews in Medicinal Chemistry 20, № 17 (2020): 1791–818. http://dx.doi.org/10.2174/1389557520666200619121003.

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α-Glucosidase plays an important role in carbohydrate metabolism and is an attractive drug target for the treatment of diabetes, obesity and other related complications. Currently, acarbose, miglitol and voglibose have been approved by the FDA for the treatment of diabetes by oral α-glucosidase inhibitors. With the development of anti-diabetic drugs, the emergence of novel drugs with various chemotypes has overshadowed α-glucosidase inhibitors. Since the 1990s, the FDA has not approved new chemical entities against α-glucosidase, which has resulted in restricted clinical medication. Neverthele

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Карпенко, Ю. В., О. І. Панасенко, and В. В. Парченко. "Evaluation of the hypoglycemic potential of 6-(4-ethyl-5-mercapto-4H-1,2,4-triazol-3-yl)pyrimidine-2,4(1H,3H)-dione derivatives." Farmatsevtychnyi zhurnal, no. 1 (February 26, 2025): 45–57. https://doi.org/10.32352/0367-3057.1.25.04.

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Type 2 diabetes mellitus is one of the most prevalent metabolic diseases worldwide, characterized by chronic hyperglycemia and the development of severe complications. A key approach to its treatment involves the use of α-glucosidase inhibitors, which slow carbohydrate absorption in the intestine and thereby reduce postprandial hyperglycemia. In the search for new biologically active compounds, 1,2,4-triazole derivatives have garnered significant interest due to their broad spectrum of pharmacological properties, including hypoglycemic activity. The aim of this study is to evaluate the potenti

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27

Lee, Sang-Hoon, Li-Yong, Fatih Karadeniz, Moon-Moo Kim, and Se-Kwon Kim. "Alpha-glucosidase and alpha-amylase inhibitory activities of phlorotannin derivatives from Ecklonia cava." Journal of Biotechnology 136 (October 2008): S588. http://dx.doi.org/10.1016/j.jbiotec.2008.07.1386.

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Heydari, Zahra, Maryam Mohammadi-Khanaposhtani, Somaye Imanparast та ін. "Pyrano[3,2-c]quinoline Derivatives as New Class of α-glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in vitro Biological Evaluation and Kinetic Study". Medicinal Chemistry 15, № 1 (2019): 8–16. http://dx.doi.org/10.2174/1573406414666180528110104.

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Background: Pyrano[3,2-c]quinoline derivatives 6a–n were synthesized via simple two-step reactions and evaluated for their in vitro α-glucosidase inhibitory activity. </P><P> Methods: Pyrano[3,2-c]quinoline derivatives 6a–n derivatives were prepared from a two-step reaction: cycloaddition reaction between 1-naphthyl amine 1 and malonic acid 2 to obtain benzo[h]quinoline-2(1H)-one 3 and reaction of 3 with aryl aldehydes 4 and Meldrum’s acid 5. The anti- α-glucosidase activity and kinetic study of the synthesized compounds were evaluated using α-glucosidase from Saccharomyces cerevis

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29

Khusnutdinova, Elmira F., Nguyen Thi Thu Ha, Gulnara V. Giniyatullina, Le Thi Tu Anh, Alexander I. Poptsov та Oxana B. Kazakova. "Synthesis and alpha ‐ inhibitory activity of lupane type С2‐benzylidene‐ triterpenoids". Vietnam Journal of Chemistry 59, № 5 (2021): 612–19. http://dx.doi.org/10.1002/vjch.202100013.

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AbstractA series of novel and previously synthesized lupane type С2‐benzylidene derivatives was evaluated on α‐glucosidase enzyme inhibition. Most of the tested compounds exhibited significantly better activity (1.8‐700 times higher) than the standard drug acarbose. The structure‐activity relationship indicated that the type of benzylidene moiety and C28‐substituent of lupane core plays an important influence on the activity. Methyl 2‐furfurylidene betulonate, m‐iodo‐benzylidene betulonic acid and 3‐pyridinylideno‐betulonic acid hydrazide have been founded as effective α‐glucosidase inhibitors

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Khokhlov, A. L., K. V. Gorelov, and J. V. Rybachkova. "To the assessment of the use of sugar-reducing drugs from the position of safety." Patient-Oriented Medicine and Pharmacy 1, no. 1 (2023): 41–48. http://dx.doi.org/10.37489/2949-1924-0006.

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The results and the degree of safety of hypoglycaemic drugs are presented. The current work analyses the safety of the use of sulfonylurea derivatives, biguanides, thiazolidinediones, meglitinides and α-glucosidase inhibitors according to clinical studies published in the scientific literature. Macrovascular complications in diabetes mellitus (DM) develop much earlier than microvascular complications and cause death in 75 % — 80 % of patients. The safety of hypoglycaemic therapy is assessed by the occurrence of hypoglycaemia, changes in body weight, effects on the gastrointestinal tract, and,

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Monroy-Cárdenas, Matías, Cristopher Almarza, Paulina Valenzuela-Hormazábal, et al. "Identification of Antioxidant Methyl Derivatives of Ortho-Carbonyl Hydroquinones That Reduce Caco-2 Cell Energetic Metabolism and Alpha-Glucosidase Activity." International Journal of Molecular Sciences 25, no. 15 (2024): 8334. http://dx.doi.org/10.3390/ijms25158334.

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α-glucosidase, a pharmacological target for type 2 diabetes mellitus (T2DM), is present in the intestinal brush border membrane and catalyzes the hydrolysis of sugar linkages during carbohydrate digestion. Since α-glucosidase inhibitors (AGIs) modulate intestinal metabolism, they may influence oxidative stress and glycolysis inhibition, potentially addressing intestinal dysfunction associated with T2DM. Herein, we report on a study of an ortho-carbonyl substituted hydroquinone series, whose members differ only in the number and position of methyl groups on a common scaffold, on radical-scaveng

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Patidar, Mohini, Raghvendra Dubey, Sunita Minz, Madhulika Pradhan, and Nitin Deshmukh. "A mechanism-driven strategy for in-silico prediction, molecular docking, synthesis, and biological assessment of substituted 1,3,4-oxadiazole derivatives as novel antidiabetic agents." Journal of Applied Pharmaceutical Research 13, no. 2 (2025): 194–203. https://doi.org/10.69857/joapr.v13i2.1031.

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Background: Diabetes mellitus is a long-standing and debilitating metabolic condition that imposes a substantial global health burden, leading to severe and widespread complications. Objectives: This study aims to predict physicochemical properties of 1,3,4-oxadiazole derivatives using in-silico methods and molecular docking simulations to explore their potential as α-glucosidase inhibitors for diabetes management. Furthermore, this study aims to experimentally synthesize and characterize these derivatives to validate their inhibitory activity. Methods: In silico drug-likeness, pharmacokinetic

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Tafesse, Tadesse Bekele, Mohammed Hussen Bule, Mehdi Khoobi, Mohammad Ali Faramarzi, Mohammad Abdollahi та Mohsen Amini. "Coumarin-based Scaffold as α-glucosidase Inhibitory Activity: Implication for the Development of Potent Antidiabetic Agents". Mini-Reviews in Medicinal Chemistry 20, № 2 (2020): 134–51. http://dx.doi.org/10.2174/1389557519666190925162536.

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Background: Delaying the absorption of glucose through α-glucosidase enzyme inhibition is one of the therapeutic approaches in the management of Type 2 diabetes, which can reduce the incidence of postprandial hyperglycemia. The existence of chronic postprandial hyperglycemia impaired the endogenous antioxidant defense by inducing oxidative stress-induced pancreatic β-cell destruction through uncontrolled generation of free radicals such as ROS, which in turn, leads to various macrovascular and microvascular complications. The currently available α -glucosidase inhibitors, for instance, acarbos

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Danova, Ade, Elvira Hermawati, Warinthorn Chavasiri, Didin Mujahidin, Anita Alni, and Robby Roswanda. "Discovery of thymol-fused chalcones as new competitive \(\alpha\)-glucosidase inhibitors: Design, synthesis, biological evaluation, and molecular modeling studies." Communications in Science and Technology 9, no. 2 (2024): 322–30. https://doi.org/10.21924/cst.9.2.2024.1497.

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This study aims to synthesize and evaluate the inhibitory activity of thymol derivatives targeting ?-glucosidase using in vitro and in silico studies. Ten thymol derivatives (2-11) including five new thymol-fused chalcones (7-11) were successfully synthesized. Among them, four compounds (4, 8, 9, 11) showed the best inhibitory activity with IC50 values of 18.45, 13.75, 8.86, and 10.67µM compared with acarbose (IC50 = 832.82 µM), respectively. The kinetic study of three new thymol-fused chalcones (8, 9, 11) exhibited a competitive inhibition. Molecular docking demonstrated the predicted interac

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YOSHIKUNI, Yoshiaki, Yohji EZURE, Takashi SETO, Kazuya MORI, Masayoshi WATANABE, and Hiroshi ENOMOTO. "Synthesis and .ALPHA.-glucosidase-inhibiting activity of a new .ALPHA.-glucosidase inhibitor, 4-O-.ALPHA.-D-glucopyranosylmoranoline and its N-substituted derivatives." CHEMICAL & PHARMACEUTICAL BULLETIN 37, no. 1 (1989): 106–9. http://dx.doi.org/10.1248/cpb.37.106.

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ALi, Hassan, Mohammed H. Mohammed, and Sajida H. Ismeal. "Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 27, no. 1 (2018): 100–108. http://dx.doi.org/10.31351/vol27iss1pp100-108.

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Three of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as the end products

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Wang, Haibo, Xiaojiang Huang, Yang Pan та ін. "Synthesis and Biological Evaluation of New Dihydrofuro[3,2-b]piperidine Derivatives as Potent α-Glucosidase Inhibitors". Molecules 29, № 5 (2024): 1179. http://dx.doi.org/10.3390/molecules29051179.

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Inhibition of glycoside hydrolases has widespread application in the treatment of diabetes. Based on our previous findings, a series of dihydrofuro[3,2-b]piperidine derivatives was designed and synthesized from D- and L-arabinose. Compounds 32 (IC50 = 0.07 μM) and 28 (IC50 = 0.5 μM) showed significantly stronger inhibitory potency against α-glucosidase than positive control acarbose. The study of the structure–activity relationship of these compounds provides a new clue for the development of new α-glucosidase inhibitors.

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Khan, Imran Ahmad, Matloob Ahmad, Usman Ali Ashfaq, Sadia Sultan та Magdi E. A. Zaki. "Discovery of Amide-Functionalized Benzimidazolium Salts as Potent α-Glucosidase Inhibitors". Molecules 26, № 16 (2021): 4760. http://dx.doi.org/10.3390/molecules26164760.

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α-Glucosidase inhibitors (AGIs) are used as medicines for the treatment of diabetes mellitus. The α-Glucosidase enzyme is present in the small intestine and is responsible for the breakdown of carbohydrates into sugars. The process results in an increase in blood sugar levels. AGIs slow down the digestion of carbohydrates that is helpful in controlling the sugar levels in the blood after meals. Among heterocyclic compounds, benzimidazole moiety is recognized as a potent bioactive scaffold for its wide range of biologically active derivatives. The aim of this study is to explore the α-glucosida

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Chandrashekhara, Kumar B* Arun A. Bhagwath Chandrashekar K. S. "Pharmaceutical Chemistry Of Anthranilic Acid Derivatives: A Brief Review." International Journal of Pharmaceutical Sciences 2, no. 7 (2024): 2143–74. https://doi.org/10.5281/zenodo.13131906.

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Anthranilic acid is a benzenoid compound that has adjacent active important two reactive groups namely carboxylic acid group (-COOH) and amino group (-NH<sub>2</sub>). Consequently fascinating anthranilic acid derivatives have been prepared through both the active functional groups.  The literature review reveals an experiential and holistic approach of various manufacturing procedures and skills used for the production of anthranilic acid analogues and anthranilic scaffold along with the biological activities of some of the promising derived anthranilic acid molecules.  Pharmacology

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Fais, Antonella, Benedetta Era, Amalia Di Petrillo, et al. "Selected Enzyme Inhibitory Effects of Euphorbia characias Extracts." BioMed Research International 2018 (May 29, 2018): 1–9. http://dx.doi.org/10.1155/2018/1219367.

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Extracts of aerial part of Euphorbia characias were examined to check potential inhibitors for three selected enzymes involved in several metabolic disorders. Water and ethanol extracts from leaves and flowers showed in vitro inhibitory activity toward α-amylase, α-glucosidase, and xanthine oxidase. IC50 values were calculated for all the extracts and the ethanolic extracts were found to exert the best effect. In particular, for the α-glucosidase activity, the extracts resulted to be 100-fold more active than the standard inhibitor. The inhibition mode was investigated by Lineweaver-Burk plot

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Phuong Thao, Tran Thi, Thanh Q. Bui, Phan Tu Quy, et al. "Isolation, semi-synthesis, docking-based prediction, and bioassay-based activity of Dolichandrone spathacea iridoids: new catalpol derivatives as glucosidase inhibitors." RSC Advances 11, no. 20 (2021): 11959–75. http://dx.doi.org/10.1039/d1ra00441g.

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Ullah, Hayat, Fazal Rahim, Muhammad Taha та ін. "Synthesis, In vitro α-Glucosidase Inhibitory Potential and Molecular Docking Studies of 2-Amino-1,3,4-Oxadiazole Derivatives". Medicinal Chemistry 16, № 6 (2020): 724–34. http://dx.doi.org/10.2174/1573406415666190612150447.

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Background: In the recent past, we have synthesized and reported different derivatives of oxadiazoles as potential α-glucosidase inhibitors, keeping in mind, the pharmacological aspects of oxadiazole moiety and in continuation of our ongoing research on the chemistry and bioactivity of new heterocyclic compounds. Methods: 1,3,4-Oxadiazole derivatives (1-14) have been synthesized and characterized by different spectroscopic techniques such as 1H-, 13C-NMR and HREI-MS. Result: The synthetic derivatives were screened for α-glucosidase inhibitory potential. All compounds exhibited good inhibitory

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Saddique, Furqan Ahmad, Matloob Ahmad, Usman Ali Ashfaq, Muhammad Muddassar, Sadia Sultan та Magdi E. A. Zaki. "Identification of Cyclic Sulfonamides with an N-Arylacetamide Group as α-Glucosidase and α-Amylase Inhibitors: Biological Evaluation and Molecular Modeling". Pharmaceuticals 15, № 1 (2022): 106. http://dx.doi.org/10.3390/ph15010106.

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Diabetes mellitus (DM), a complicated metabolic disorder, is due to insensitivity to insulin function or reduction in insulin secretion, which results in postprandial hyperglycemia. α-Glucosidase inhibitors (AGIs) and α-amylase inhibitors (AAIs) block the function of digestive enzymes, which delays the carbohydrate hydrolysis process and ultimately helps to control the postprandial hyperglycemia. Diversified 2-(3-(3-methoxybenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides were synthesized and evaluated for their in vitro inhibitory potential against α-glucosidase an

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Taha, Muhammad, Nor Hadiani Ismail, Syahrul Imran та ін. "Novel quinoline derivatives as potent in vitro α-glucosidase inhibitors: in silico studies and SAR predictions". MedChemComm 6, № 10 (2015): 1826–36. http://dx.doi.org/10.1039/c5md00280j.

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Sevšek, Alen, Javier Sastre Toraño, Linda Quarles van Ufford, Ed E. Moret, Roland J. Pieters та Nathaniel I. Martin. "Orthoester functionalizedN-guanidino derivatives of 1,5-dideoxy-1,5-imino-d-xylitol as pH-responsive inhibitors of β-glucocerebrosidase". MedChemComm 8, № 11 (2017): 2050–54. http://dx.doi.org/10.1039/c7md00480j.

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Zeng, Yin, Chen та ін. "Design, Synthesis, and Activity Evaluation of Novel N-benzyl Deoxynojirimycin Derivatives for Use as α-Glucosidase Inhibitors". Molecules 24, № 18 (2019): 3309. http://dx.doi.org/10.3390/molecules24183309.

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To obtain α-glucosidase inhibitors with high activity, 19 NB-DNJDs (N-benzyl-deoxynojirimycin derivatives) were designed and synthesized. The results indicated that the 19 NB-DNJDs displayed different inhibitory activities towards α-glucosidase in vitro. Compound 18a (1-(4-hydroxy-3-methoxybenzyl)-2-(hydroxymethyl) piperidine-3,4,5-triol) showed the highest activity, with an IC50 value of 0.207 ± 0.11 mM, followed by 18b (1-(3-bromo-4-hydroxy-5-methoxybenzyl)-2-(hydroxymethyl) piperidine-3,4,5-triol, IC50: 0.276 ± 0.13 mM). Both IC50 values of 18a and 18b were significantly lower than that of

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Shahzad, Danish, Aamer Saeed, Fayaz Ali Larik та ін. "Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics". Molecules 24, № 8 (2019): 1511. http://dx.doi.org/10.3390/molecules24081511.

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A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a–5h, have been synthesized, characterized by 1H-NMR and 13C-NMR, and evaluated for their in vitro α-glucosidase and α-amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both α-glucosidase and α-amylase. The IC50 of 5g against α-glucosidase was 0.35917 ± 0.0189 µM (standard acarbose IC50 = 6.109 ± 0.329 µM), and the IC50 value of 5g against α-amylase was 0.4379 ± 0.0423 µM (standard acarbose IC50 =

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Shen, Qiong, Jialiang Shao, Quan Peng та ін. "Hydroxycoumarin Derivatives: Novel and Potent α-Glucosidase Inhibitors". Journal of Medicinal Chemistry 53, № 23 (2010): 8252–59. http://dx.doi.org/10.1021/jm100757r.

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Pluempanupat, Wanchai, Sirichai Adisakwattana, Sirintorn Yibchok-Anun та Warinthorn Chavasiri. "Synthesis ofN-phenylphthalimide Derivatives as α-Glucosidase Inhibitors". Archives of Pharmacal Research 30, № 12 (2007): 1501–6. http://dx.doi.org/10.1007/bf02977317.

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Hu, Wei-ping, Guo-dong Cao, Jin-hua Zhu, Jia-zhong Li та Xiu-hua Liu. "Naturally occurring Batatasins and their derivatives as α-glucosidase inhibitors". RSC Advances 5, № 100 (2015): 82153–58. http://dx.doi.org/10.1039/c5ra15328j.

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