Diabetes and Health Care: An Overview

M, Abhilash; Augustine, Robin

doi:10.1201/b16415-6

Cited by 1 publication

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“…It has been documented that novel 2,4-thiazolidinedione derivatives (TZDs) have emerged as an important pharmacologically active class and have a special place in drug design and discovery [8]. Compounds belonging to this class of heterocyclic compounds are being successfully used in various diabetic complexities and for the patients of Type-2 Diabetes [9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, α-Amylase Inhibitory Activity and Molecular Docking Studies of 2,4-Thiazolidinedione Derivatives

Naeem¹,

Nadeem²,

Muhammad³

et al. 2018

CHEM

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Introduction: 2,4-Thiazolidinedione and its derivatives exhibit a variety of pharmacological activities including antidiabetic, antiviral, antifungal, anti-inflammatory, anti-cancer and aldose reductase inhibitory activities. Keeping in mind the pharmacological potential of 2,4-Thiazolidinedione derivatives as antidiabetic agents, seven arylidene derivatives of 2,4-thiazolidinedione 1(a-g) and four corresponding acetic acid derivatives 2(a-d) have been synthesized by a three-step procedure. Methods: All the synthesized compounds were characterized by elemental analysis, FTIR, 1HNMR, and 13CNMR and further screened for their α-amylase inhibitory potential. Results: All the compounds 1(a-g) and 2(a-d) showed varying degree of α-amylase inhibition, especially compound 1c (IC50 = 6.59μg/ml), 1d (IC50=2.03μg/ml) and 1g (IC50 = 3.14μg/ml) displayed significantly potent α-amylase inhibition as compared to the standard acarbose (IC50 = 8.26μg/ml). None of the acetic acid derivatives of 5-arylidene-2,4-thiazolidinedione showed prominent inhibitory activity. Docking results indicated that the best binding conformation was found inside the active site cleft of enzyme responsible for hydrolysis of carbohydrates. Conclusion: Therefore, it can be concluded that 2,4-thiazolidinedione derivatives can be used as effective lead molecules for the development of α-amylase inhibitors for the management of diabetes.

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Section: Introductionmentioning

confidence: 99%