Synthesis, molecular docking study of thiazole derivatives and exploring their dual inhibitor potentials against α-amylase and α-glucosidase

Ullah, Hayat; Ahmad, Nisar; Uddin, Imad; Hayat, Shawkat; Zada, Hussan; Zaman, Khalid; Farooqi, Kamran; Bakhtiar, Manahil; Khan, Irshad Ullah; Rehman, Ashfaq Ur; Wadood, Abdul

doi:10.1016/j.cdc.2022.100932

Cited by 18 publications

(6 citation statements)

References 42 publications

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“…[10] Benzothiazole contains fused benzene with the five membered thiazole rings. Benzothiazole is an afuent endocyclic ring system with multiple biological activities that includes anticancer, [11] anti-diabetic, [12] anti-inflammatory, [13] anti-viral [14] and anti-tuberculosis. [15] Thiazole is an organic heterocyclic compound having five membered heterocyclic ring of three carbons, one nitrogen and sulphur atom.…”

Section: Introductionmentioning

confidence: 99%

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Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach

Ullah,

Alam,

Zainab

et al. 2024

ChemistrySelect

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This research work is based on synthesis of eleven novel thiazole derivatives (3 a‐k) of thiophene carbaldehyde. All the synthesized compounds were successfully synthesized, characterized by 1H‐NMR and EI‐MS spectroscopic techniques and finally subjected for their in vitro α‐glucosidase inhibitory activity. Seven derivatives 3 i (IC50=10.21±1.84 μM), 3 b (IC50=11.14±0.99 μM), 3 f (IC50=13.21±2.76 μM), 3 h (IC50=14.21±0.31 μM), 3 k (IC50=15.21±1.02 μM), 3 e (IC50=16.21±1.32 μM), and 3 c (IC50=18.21±1.89 μM), in the series displayed excellent inhibitory potential better than the standard acarbose. However, two compounds 3 g (IC50=33.21±1.99 μM) and 3 d (IC50=42.31±2.12 μM) showed significant activity while two compounds 3 j and 3 a were found less active with IC50 values of 82.31±0.31 and 88.36±1.21 μM respectively. Additional research revealed that the compounds are not exhibiting any cytotoxic effects. The molecular docking study of these derivatives showed their good binding potential for α‐glucosidase active site with excellent interactions and docking scores.

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Section: Introductionmentioning

confidence: 99%

“…Benzothiazole contains fused benzene with the five membered thiazole rings. Benzothiazole is an afuent endocyclic ring system with multiple biological activities that includes anticancer, [11] anti‐diabetic, [12] anti‐inflammatory, [13] anti‐viral [14] and anti‐tuberculosis [15]…”

Section: Introductionmentioning

confidence: 99%

Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach

Ullah,

Alam,

Zainab

et al. 2024

ChemistrySelect

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“…Compound 10 (Figures 5 and 6) exhibited potent inhibitory activity with IC 50 : 0.6±0.05 μM and IC 50 : 0.50±0.05 μM than standard acarbose IC 50 : 8.90±0.10 μM and IC 50 : 9.10±0.10 μM and for all derivatives, the structural activity relationship (SAR) has been developed. SAR is mostly dependent on the type, position, and number of substituent(s) on the phenyl ring [19] …”

Section: Discussionmentioning

confidence: 99%

“…SAR is mostly dependent on the type, position, and number of substituent(s) on the phenyl ring. [19] Angajala G et al studied by employing the MK-10 catalyst for Knoevenagel condensation, rhodanine acridine derivatives were created and then further screened for inhibitory acitivity like α-amylase and α-glucosidase. Compound 11 exhibited potent inhibitory activity with IC 50 : 85.24 � 1.06 and 87.18 � 0.90 as compared to standard and molecular modeling, molecular docking, and SAR ascribed to the presence of piperidine ring and presence of electron withdrawing groups namely À Cl group at 2' position which is biologically more potent.…”

Section: Pharmacological Characteristics Of Thiazole Analoguesmentioning

confidence: 99%

Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Gharge,

Alegaon

2024

Chemistry & Biodiversity

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The prevalence of diabetes mellitus is on the rise, which demands for the identification of novel antidiabetic drugs. There is a need for safer and more effective alternatives because the therapy methods now available to manage diabetes have limits. Due to their diverse pharmacological characteristics, heterocyclic molecules with nitrogen and Sulfur atoms have become intriguing candidates in medicinal chemistry. These substances have a wide variety of structures that can be customized to target different pathways associated with diabetes and can affect important biological targets involved in glucose homeostasis. This review provides a thorough summary of the most recent studies on heterocyclic analogues of nitrogen and Sulfur as prospective antidiabetic agents. This review examines the variety of their structural forms, their methods of action, and assesses the results of preclinical and clinical investigations on their effectiveness and safety. Additionally, further optimization and development of innovative antidiabetic medications are highlighted, as well as the difficulties and prospects for the future in utilizing the therapeutic potential of these analogues. This study seeks to stimulate additional investigation and cooperation between researchers and medicinal chemists, promoting improvements in the creation of efficient and secure antidiabetic medicines to fulfil the needs in the management of diabetes.

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“…This disease results in disturbances in carbohydrate, protein, and fat metabolism due to hormone secretion and insulin deficiency. 27 Early diagnosis and appropriate treatment methods are crucial to reducing the burden of diabetes on both individuals and society. As a result, research on the suppression of diabetic complications is gaining importance.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of amantadine clubbed N-aryl amino thiazoles as potent urease, α-amylase & α-glucosidase inhibitors, kinetic and molecular docking studies

Zahra,

Saeed,

Ahmed

et al. 2023

RSC Adv.

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Synthesis, molecular docking study of thiazole derivatives and exploring their dual inhibitor potentials against α-amylase and α-glucosidase

Cited by 18 publications

References 42 publications

Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach

Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach

Recent Studies of Nitrogen and Sulfur Containing Heterocyclic Analogues as Novel Antidiabetic Agents: A Review

Synthesis of amantadine clubbed N-aryl amino thiazoles as potent urease, α-amylase & α-glucosidase inhibitors, kinetic and molecular docking studies

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