Design, synthesis and bioactivity evaluation of thiazolidinedione derivatives as partial agonists targeting PPARγ

Sun, Juan; Liu, Hanyu; Zhang, Yiheng; Fang, Ze-Yu; Lv, Peng‐Cheng

doi:10.1016/j.bioorg.2021.105342

Cited by 10 publications

(2 citation statements)

References 33 publications

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“…The molecular docking study revealed hydrogen bond interaction between TYR473 and compound 92, and the competitive binding assay confirmed compound 92 direct binding to PPAR-γ with an IC 50 of 1790 nm. [102] Saeedian Moghadam E et. Studied 5-benzylidene-2,3-diarylthiazolidine-4one derivatives and evaluated for their ability to inhibit αglucosidase.…”

Section: Pharmacological Characteristics Of Thiazolidine 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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Section: Pharmacological Characteristics Of Thiazolidine 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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“…Therapy selection is individualized for each patient, which makes the search for new classes of hypoglycemic agents an important task [8]. New hypoglycemic agents are being scouted both for known targets, such as dipeptidyl peptidase-4 (DPP4) inhibitors [9,10], thiazolidinediones [11,12], α-glycosidase inhibitors [13][14][15], and sodium-glucose linked transporter-2 (SGLT-2) inhibitors [16,17], as 2 of 16 well as for new targets with no approved drugs yet available. A fairly new target for the creation of hypoglycemic agents is free fatty acid receptor-1 (FFAR1), previously known as GPR40.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Hypoglycemic Activity of Structural Isomers of ((Benzyloxy)phenyl)propanoic Acid Bearing an Aminobornyl Moiety

Kuranov

Pon`kina

Meshkova

et al. 2023

IJMS

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Free fatty acid receptor-1 (FFAR1) agonists are promising candidates for therapy of type 2 diabetes because of their ability to normalize blood sugar levels during hyperglycemia without the risk of hypoglycemia. Previously, we synthesized compound QS-528, a FFA1 receptor agonist with a hypoglycemic effect in C57BL/6NCrl mice. In the present work, structural analogs of QS-528 based on (hydroxyphenyl)propanoic acid bearing a bornyl fragment in its structure were synthesized. The seven novel compounds synthesized were structural isomers of compound QS-528, varying the positions of the substituents in the aromatic fragments as well as the configuration of the asymmetric center in the bornyl moiety. The studied compounds were shown to have the ability to activate FFAR1 at a concentration of 10 μM. The cytotoxicity of the compounds as well as their effect on glucose uptake in HepG2 cells were studied. The synthesized compounds were found to increase glucose uptake by cells and have no cytotoxic effect. Two compounds, based on the meta-substituted phenylpropanoic acid, 3-(3-(4-(((1R,2R,4R)-1,7,7-trimethylbicyclo-[2.2.1]heptan-2-ylamino)methyl)benzyloxy)phenyl)propanoic acid and 3-(3-(3-(((1R,2R,4R)-1,7,7-trimethylbicyclo [2.2.1]heptan-2-ylamino)methyl)benzyloxy)phenyl)propanoic acid, were shown to have a pronounced hypoglycemic effect in the oral glucose tolerance test with CD-1 mice.

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Antidiabetic potential of thiazolidinedione derivatives with efficient design, molecular docking, structural activity relationship, and biological activity: an update review (2021–2023)

Sharma,

Kumar,

Gulati

et al. 2024

Mol Divers

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Design, synthesis and bioactivity evaluation of thiazolidinedione derivatives as partial agonists targeting PPARγ

Cited by 10 publications

References 33 publications

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

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

Synthesis and Evaluation of Hypoglycemic Activity of Structural Isomers of ((Benzyloxy)phenyl)propanoic Acid Bearing an Aminobornyl Moiety

Antidiabetic potential of thiazolidinedione derivatives with efficient design, molecular docking, structural activity relationship, and biological activity: an update review (2021–2023)

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