Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents

Datar, Prasanna A.; Aher, Sainath Babaji

doi:10.1016/j.jscs.2012.10.010

Cited by 30 publications

(12 citation statements)

References 14 publications

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“…Mechanisms of action include diminution of free fatty acid accumulation, reduction in inflammatory cytokines, rising adiponectin levels, and preservation of ß-cell integrity and function, all leading to improvement of insulin resistance and ß-cell exhaustion. TZDs selectively enhance or partially mimic certain actions of insulin, causing a slowly generated anti hyperglycemic effect in Type 2 diabetic patients [12].…”

Section: Thiazolidinedionementioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of Thiazolidinedione Derivative as Novel Antidiabetic Agents

Patel¹,

Sen²,

Dash³

et al. 2021

JPRI

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Thiazolidinedione derivative have Antihyperglycemic activity, they are agonists for the peroxisome proliferator-activated receptor (PPAR), which controls glucose synthesis, transport, and utilization via regulating the transcription of insulin-responsive genes. A number of novel insulin sensitizers are currently being researched. Several of these are derivatives of Thiazolidinedione, but others have different chemical structures. In this work, we created some new Thiazolidinedione derivative based on structure–activity relationship as closely as feasible. The Thiazolidine-2,4-Dione derivatives were manually developed and synthesized using the proper synthetic techniques, then tested in vitro for antihyperglycemic action using the Sucrose loading model (SLM) and the Alloxan induced diabetes model (AIDM). The newly synthesized Thiazolidine-2,4-Dione derivative was characterized using infrared (IR) and proton (H) nuclear magnetic resonance. In this study we found that Compound M-4 has a lot of antihyperglycemic action, thus it's a good idea to think about using it as a lead material for the creation of anti-diabetic drugs.

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Section: Thiazolidinedionementioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of Thiazolidinedione Derivative as Novel Antidiabetic Agents

Patel¹,

Sen²,

Dash³

et al. 2021

JPRI

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“…Ser-289, His-323, His-449, and Tyr-473 (Fig. 3) contributes the important amino acid residues around binding pocket that allow hydrogen bonding with carboxylic acids of natural modulators or keto group of synthetic agonist thiazolidinediones (TZDs) [41][42][43].…”

Section: Ppar-γ -Structural Insightmentioning

confidence: 99%

Peroxisome Proliferator-Activated Receptor-Gamma, an Emerging Potential Target to Combat Metabolic Disorder

Bairy¹

2017

Asian J Pharm Clin Res

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Day-by-day metabolic disorder/syndrome (MS) falling in love with current lifestyle status of everyone especially after study age group of people. If we look carefully around us, we will see evidence is growing up of diabetic, obese, and hypertensive population regularly. In urgencies of above view extensive literature survey has been done prioritizing prevalence of metabolic disorder and peroxisome proliferator-activated receptor-gamma (PPAR-γ) as potential target protein. This review covered current status of MS emphasizing diabetes along with its management criteria. Special importance is given to PPAR-γ exploring its metabolic regulation and structural orientation for understanding ligand-protein interaction. Development of PPAR-γ agonist thiazolidinediones (TZDs) and other pharmacodynamic importance of this nuclear receptor also discussed. Being as nuclear receptor more genomics exploitation needs to be done emphasizing minimization of cardiac adverse effect. Selective PPAR modulator (SPPRM), TZDs are the master regulator of adipogenesis and angiogenesis which makes TZD more interesting topic to explore. Developmental hierarchy suggests that in a few years from now PPAR-γ won't be in the list of double edge sword.

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“…The presence of size and type of ring structures, having different dominant substituents showed their physiochemical properties [1–2] and they are known so far for their utilities. Most of the heterocyclic compounds used in form of drugs as anti‐tumour, antihistaminics, anticonvulsants, antineoplastics, hypnotics, antiseptics, antimicrobial, [3–5] anti‐inflammatory, [6] antioxidant, [7] anticancer, [8–10] antidiabetic, [11] antitrypanosomal, [12] antiparasitic, [13] anti‐tumour, [14] neuroprotective, [15] antiproliferative, [16] anti‐obesity, [17] antihyperglycemic, [18] antihypercholesteroler, [19] antiulcer, [20] antileishmanial, [21] antibiotic, [22] etc . The development of recent methodologies for organic and heterocyclic synthesis is considered a successful pathway for synthetic chemists which is also useful to prepare the chemicals in bulk amounts.…”

Section: Introductionmentioning

confidence: 99%

Recent advances in the synthesis of five‐ and six‐membered heterocycles as bioactive skeleton: A concise overview

et al. 2022

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Heterocyclic compounds play a tremendous role in the field of medicinal chemistry due to their association with diverse pharmacological properties. Most of the pharmaceutical drugs used in medicines possess a wide range of heterocyclic nucleus. It was decided basis on literature studies that various synthetic protocols like microwave‐assisted, nanocatalysed, green synthesis, click reaction, and multicomponent routes could be used for the betterment of the purity of products, selectivity, and better yields of the products. We have focused attention on the development of synthetic strategies of the above‐mentioned moieties because N‐, O‐ and S‐ containing heterocyclic compounds have seemed owing to a wide diversity of their biological activities viz. antioxidant, anticancer, anticonvulsant, anti‐inflammatory, neuroprotective, antiproliferative, anti‐obesity, antihyperglycemic, antihypercholesteroler, antiulcer, antidiabetic, antileishmanial, antitrypanosomal, antibiotic, etc. In this review article, an overview of the applications of synthetic protocols for the preparation of five‐membered and six‐membered heterocyclic compounds containing two or more heteroatoms (O, N, S) at different‐different positions along with their different potent and competent candidates against various diseases is presented in last 10–15 years.

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Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents

Cited by 30 publications

References 14 publications

Synthesis, Characterization and Biological Evaluation of Thiazolidinedione Derivative as Novel Antidiabetic Agents

Synthesis, Characterization and Biological Evaluation of Thiazolidinedione Derivative as Novel Antidiabetic Agents

Peroxisome Proliferator-Activated Receptor-Gamma, an Emerging Potential Target to Combat Metabolic Disorder

Recent advances in the synthesis of five‐ and six‐membered heterocycles as bioactive skeleton: A concise overview

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