Multicomponent reaction for the synthesis of new 1,3,4-thiadiazole-thiazolidine-4-one molecular hybrids as promising antidiabetic agents through α-glucosidase and α-amylase inhibition

Gummidi, Lalitha; Kerru, Nagaraju; Ebenezer, Oluwakemi; Awolade, Paul; Sanni, Olakunle; Islam, Md. Shahidul; Singh, Parvesh

doi:10.1016/j.bioorg.2021.105210

Cited by 36 publications

(27 citation statements)

References 52 publications

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“…These enzymes are recognized as targets for modulating the postprandial hyperglycemia (Yang & Kong, 2016), maintaining the overall body glucose levels (Gummidi et al, 2021), and they are present in several plant species due to their bioactive compounds (de Sales et al, 2012).…”

Section: Diabetesmentioning

confidence: 99%

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

Cisneros‐Yupanqui

Lante

Mihaylova

et al. 2022

Food Bioprocess Technol

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The concept of functional foods is gaining more importance due to its role in maintaining a healthy status and preventing some metabolic diseases. The control of diabetes, in particular type-2 (T2DM), could be considered a big challenge since it involves other factors such as eating habits. From the pharmacological point of view, inhibiting digestive enzymes, such as α-amylase and α-glucosidase, is one of the mechanisms mainly used by synthetic drugs to control this disease; however, several side effects are described. For that reason, using bioactive compounds may appear as an alternative without presenting the complications synthetic drugs available on the market have. The winemaking industry generates tons of waste annually, and grape pomace (GP) is the most important. GP is recognized for its nutritional value and as a source of bioactive compounds that are helpful for human health. This review highlights the importance of GP as a possible source of α-amylase and α-glucosidase inhibitors. Also, it is emphasized the components involved in this bioactivity and the possible interactions among them. Especially, some phenolic compounds and fiber of GP are the main ones responsible for interfering with the human digestive enzymes. Preliminary studies in vitro confirmed this bioactivity; however, further information is required to allow the specific use of GP as a functional ingredient inside the market of products recommended for people with diabetes. Graphical abstract

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Section: Diabetesmentioning

confidence: 99%

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

Cisneros‐Yupanqui

Lante

Mihaylova

et al. 2022

Food Bioprocess Technol

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“…Considered among the most biologically promising nitrogenous five-membered heterocycles. They comprised a wide-ranging library of drug categories [4] , [5] , [6] , [7] , [8] , [9] , [10] , [11] , [12] , [13] , [14] , [15] like, anti-inflammatory, antidiabetic [ 16 , 17 ], antimicrobial [ 11 , 14 ], anticancer [ 6 , 15 , [18] , [19] , [20] , [21] ], antiviral [4] , antileishmanial [22] , etc.…”

Section: Introductionmentioning

confidence: 99%

Towards Covid-19 TMPRSS2 enzyme inhibitors and antimicrobial agents: Synthesis, antimicrobial potency, molecular docking, and drug-likeness prediction of thiadiazole-triazole hybrids

Rashdan¹,

Abdelmonsef²

2022

Journal of Molecular Structure

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“…Thiazolidine-4-ones also have extensive biological activities, anti-bacterial, anticancer and anti-inflammatory HIV-inhibitors [6]. Thiazolidines are a key breakthrough in diabetes treatment because they increase insulin sensitivity [7]. So it is also called "insulin sensors" when PPAR γ is activated by binding to thiazolidin, its receptor where it is left in DNA to activate a number of specific genes that eventually boost the target tissue of allergies [8].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and antibacterial activity of thiazolidine-4-one and imidazolidine-4-one derived from Mesalazine drug by microwave method

Shehab

Rasheed

2022

ijhs

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The Schiff bases (A1- A5) were produced from the reaction of the 5-aminosalicylic acid with a variety of aldehydes by microwave method. Schiff bases were reacted with thioglycolic acid to obtain thiazolidine-4-one compounds (A6 – A10). Imidazolidine-4-one compounds (A11 - A15) were prepared from the prepared Schiff bases with the amino acid (alanine). Spectroscopic methods were used to diagnose the produced compounds (IR, 1H-NMR). The biological activity against two types of bacteria Proteus mirabilis –GVe and Enterococcus faecalis +GVe have tested and compared with the Mesalazine drug. The results proved that some of the prepared compounds are effective against these bacteria at different concentrations of 5 mg/ml, 10 mg/ml, and 15 mg/ml.

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Multicomponent reaction for the synthesis of new 1,3,4-thiadiazole-thiazolidine-4-one molecular hybrids as promising antidiabetic agents through α-glucosidase and α-amylase inhibition

Cited by 36 publications

References 52 publications

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

Towards Covid-19 TMPRSS2 enzyme inhibitors and antimicrobial agents: Synthesis, antimicrobial potency, molecular docking, and drug-likeness prediction of thiadiazole-triazole hybrids

Synthesis, characterization and antibacterial activity of thiazolidine-4-one and imidazolidine-4-one derived from Mesalazine drug by microwave method

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