Synthesis and characterization of thiazolidine-4-one compounds derived from chalcone and evaluation of the biological activity of some of them

Taha, Souad Thamer; Karim, Mohamed G. Abdel; Jassim, Saad Salem

doi:10.1016/j.matpr.2021.09.081

Cited by 2 publications

(1 citation statement)

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“…[ 26‐29 ] Owing to the diverse range of biological activities like antidiabetic, anti‐inflammatory, anticancer, antifungal, antibacterial, antioxidant, and antihypertensive activities, etc., medicinal chemists have recently exploited this nucleus to design and develop potential novel compounds. [ 29‐37 ] Thiazolidine nucleus is a 5‐membered saturated ring having a thioether and an amine group at the 1st and 3rd positions, respectively as illustrated in Figure 1. It holds three possible positions for substitution that is, 2nd, 3rd and 5th which allows it to form a large number of derivatives on chemical modification.…”

Section: Introductionmentioning

confidence: 99%

A comprehensive review on the antidiabetic attributes of thiazolidine‐4‐ones: Synthetic strategies and structure–activity relationships

Pradhan

Gupta

Kumar

et al. 2022

Archiv der Pharmazie

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The thiazolidine-4-one scaffold has recently emerged as a potential pharmacophore having clinical significance for medicinal chemists. This heterocyclic ring has been reported to possess a plethora of biological activities, including antidiabetic activity that has inspired researchers to integrate this core with different pharmacophoric fragments to design novel and effective antidiabetic leads. The antidiabetic activity has been observed due to the ability of the thiazolidine-4-one nucleus to interact with different biological targets, including peroxisome proliferator-activated receptor γ, protein tyrosine phosphatase 1B, aldose reductase, α-glucosidase, and α-amylase. The present review discusses the mode of action of thiazolidine-4-ones through these antidiabetic drug targets. This review attempts to summarize and analyze the recent developments with regard to the antidiabetic potential of thiazolidine-4-ones covering different synthetic strategies, structure-activity relationships, and docking studies reported in the literature. The significance of various structural modifications at C-2, N-3, and C-5 of the thiazolidine-4-one ring has also been discussed in this manuscript. This comprehensive compilation will provide an inevitable scope for the design and development of potential antidiabetic drug candidates having a thiazolidine-4-one core.

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Section: Introductionmentioning

confidence: 99%