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Journal articles on the topic '4-thiazolidinedione'

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Published: 4 June 2021

Last updated: 26 July 2025

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1

Chawla, P., Garg P, Panjwani D, and S. A. Saraf. "Synthesis of Some Novel 5-Substituted Arylidene – 2, 4 –Thiazolidinediones as Bioactive Agents." International Journal of Pharmaceutical Sciences and Nanotechnology 4, no. 1 (2011): 1373–78. http://dx.doi.org/10.37285/ijpsn.2011.4.1.10.

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A series of 5-substituted arylidine-2, 4-thiazolidinediones derivatives were synthesized from 2, 4-thiazolidinedione and substituted aromatic aldehydes. The synthesized title compounds were screened for their in-vivo anti-inflammatory and analgesic and in-vitro antioxidant activities as per standard protocols. All the compounds were found to possess significant activities

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Kaválek, Jaromír, Vladimír Macháček, and Vojeslav Štěrba. "Coupling Kinetics of 4-Sulfobenzenediazonium Ion with 2,4-Thiazolidinedione, Its 3-Methyl Derivative and 3-Methyl-5-isoxazolone." Collection of Czechoslovak Chemical Communications 59, no. 9 (1994): 2022–28. http://dx.doi.org/10.1135/cccc19942022.

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3- and 4-substituted 5-phenylazo derivatives of 2,4-thiazolidinedione were prepared as potential biologically active fungicides. The kinetics of coupling of 4-sulfobenzenediazonium salt with 2,4-thiazolidinedione and 3-methyl-2,4-thiazolidinedione have been studied and the results have been compared with kinetic data of coupling reaction of 3-methyl-5-isoxazolone.

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3

Klopper, Joshua P., William R. Hays, Vibha Sharma, Margaret A. Baumbusch, Jerome M. Hershman та Bryan R. Haugen. "Retinoid X receptor-γ and peroxisome proliferator-activated receptor-γ expression predicts thyroid carcinoma cell response to retinoid and thiazolidinedione treatment". Molecular Cancer Therapeutics 3, № 8 (2004): 1011–20. http://dx.doi.org/10.1158/1535-7163.1011.3.8.

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Abstract Poorly differentiated, metastatic thyroid cancer is difficult to treat. These tumors often do not concentrate radioactive iodine and may require chemotherapy, which is suboptimal and toxic. Nuclear hormone receptors peroxisome proliferator-activated receptor γ (PPARγ) and retinoid X receptor (RXR) are variably expressed in thyroid carcinoma cell lines. Expression of these receptors may predict thyroid cancer cell response to treatment with rexinoids and thiazolidinediones. We studied three thyroid carcinoma cell lines: BHP 5-16 (PPARγ−/RXRγ+), BHP 2-7 (PPARγ±/RXRγ−), and DRO-90 (RXRγ+

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4

Maji, Deepanwita, Subir Samanta, and Vaishali M. Patil. "In Silico ADMET and Docking Studies of Thiazolidinedione-acetic-acid Hybrids as Antidiabetics with Cardioprotection." Letters in Drug Design & Discovery 17, no. 12 (2020): 1475–84. http://dx.doi.org/10.2174/1570180817999200618103328.

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Background: Type-2-diabetes mellitus is associated with many side effects affecting vital body organs, especially heart. Thiazolidinediones are potent antidiabetics. Studies have proven that amino-acids and peptides promote glucose transport, have antioxidant properties, and fewer side effects, thus we designed hybrids by combining amino-acid esters and peptide esters with 2, 4 thiazolidinedione acetic acid moiety which can act as antidiabetic agent with cardioprotection properties. Methodology: In vitro ADME, toxicity, and docking studies were performed using Qikprop3.1.OSIRIS, PROTOX (Predic

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Wilmsen, Hubertina M., Theodore P. Ciaraldi, Leslie Carter, Nabeela Reehman, Sunder R. Mudaliar, and Robert R. Henry. "Thiazolidinediones upregulate impaired fatty acid uptake in skeletal muscle of type 2 diabetic subjects." American Journal of Physiology-Endocrinology and Metabolism 285, no. 2 (2003): E354—E362. http://dx.doi.org/10.1152/ajpendo.00491.2001.

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We examined the regulation of free fatty acid (FFA, palmitate) uptake into skeletal muscle cells of nondiabetic and type 2 diabetic subjects. Palmitate uptake included a protein-mediated component that was inhibited by phloretin. The protein-mediated component of uptake in muscle cells from type 2 diabetic subjects (78 ± 13 nmol · mg protein-1 · min-1) was reduced compared with that in nondiabetic muscle (150 ± 17, P < 0.01). Acute insulin exposure caused a modest (16 ± 5%, P < 0.025) but significant increase in protein-mediated uptake in nondiabetic muscle. There was no significant insu

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Chavan, Rajashree, Komal Chandhere та Ashok Bhosale. "Design, Synthesis, Biological Evaluation of Tnf-α Inhibi- Tors As Antidiabetic Agents". PDEAS International Journal of Research in Ayurved and Allied Sciences 1, № 1 (2019): 11–17. https://doi.org/10.63778/pdeasijraas-arjcpl/2019_21511.

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The weight loss in obese patients is associated with reduced Tumor necrosis factor-α (TNF-α) production and ameliorated insulin resistance. TNF-α has been shown to be an important mediator of insulin resistance linked to obesity. TNF-α interferes with insulin-signaling by inhibiting tyrosine kinase activity of the insulin receptor and the serine phosphorylation of insulin receptor substrate-1 (IRS-1). Thiazolidinediones serve as a boom in the antidiabetic therapy by increasing the sensitivity of insulin receptors towards insulin. The present study aims at designing novel thiazolidinediones wit

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Pinson, Jo-Anne, Oleg Schmidt-Kittler, Mark Frazzetto, et al. "Synthesis and Pharmacological Evaluation of 4-Iminothiazolidinones for Inhibition of PI3 Kinase." Australian Journal of Chemistry 65, no. 10 (2012): 1396. http://dx.doi.org/10.1071/ch12140.

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The thiazolidinedione, compound 1, has previously shown pan-inhibition of the phosphoinositide 3-kinase (PI3K) class I isoforms. We hypothesized the derivatization of the thiazolidinedione core of compound 1 could introduce isoform selectivity. We report the synthesis, characterization, and inhibitory activity of a novel series of 4-iminothiazolidin-2-ones for inhibition of the class I PI3K isoforms. Their synthesis was successfully achieved by multiple pathways described in this paper. Initial in vitro data of 28 analogues demonstrated poor inhibition of all class I PI3K isoforms. However, we

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Yakubu-Madus, F. E., T. W. Stephens, and W. T. Johnson. "Lipid lowering explains the insulin sensitivity enhancing effects of a thiazolidinedione, 5-(4-(2-(2-phenyl-4-oxazolyl)ethoxy)benzyl)-2,4 thiazolidinedione*." Diabetes, Obesity and Metabolism 2, no. 3 (2000): 155–63. http://dx.doi.org/10.1046/j.1463-1326.2000.00075.x.

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Bannunah, Azzah M., Naeem Fqusty, Bayan Tayeb Bokhari, Saad Alghamdi, Waheeb Alharbi, and Mohammad Asif. "Synthesis and in vitro antihyperglycemic evaluation of some new 3-(4-ethyl-6-methyl pyrimidin-2-yl)-2-arylthiazolidin-4-one derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 85. https://doi.org/10.59467/ijhc.2025.35.85.

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Due to the pharmacological potential of thiazolidinedione derivatives as antidiabetic drugs, six pyrimidine hybrids of aryl thiazolidin-4-ones (2a-f) were synthesized in two steps. In the first step, 4-ethyl-6-methyl-pyrimidin-2-amine (1) was synthesized by reacting 1,3-hexane-2,4-dione with guanidine. Compound 1 reacted with appropriate aryl aldehyde and mercaptoacetic acid to form compounds 2a-f. All the compounds (2a-f) exhibited varying degrees of a-amylase inhibitory activity, particularly compounds 2b (IC50 = 25 μg/mL), 2f (IC50 = 30 μg/mL), 2a and 2c (IC50 = 35 μg/mL) exhibited consider

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Zvarec, Ondrej, Steven W. Polyak, William Tieu, et al. "5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials." Bioorganic & Medicinal Chemistry Letters 22, no. 8 (2012): 2720–22. http://dx.doi.org/10.1016/j.bmcl.2012.02.100.

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Chis, Irina C., Doina Baltaru, Simona Clichici, Ovidiu Oniga, Ileana Cojocaru, and Cristina Nastasa. "The Effects of a 5-Chromene-yl-thiazolidin-2,4-dione Derivative in Alleviating Oxidative Stress in Adjuvant-Induced Arthritis." Revista de Chimie 69, no. 9 (2018): 2361–65. http://dx.doi.org/10.37358/rc.18.9.6534.

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Rheumatoid arthritis (RA) is a chronic inflammatory disease that reduces life quality and requires long-life therapy. Quercetin (Que) is a natural flavonoid with antioxidant and anti-inflammatory effects. (3-(2-(4-Chlorophenyl)-2-oxoethyl)-5-((6-methyl-4-oxo-4H-chromen-3-yl)methylene) thiazolidine-2,4-dione (TZD) is a thiazolidinedione derivative synthesized in our laboratory. This study was designed to investigate the antioxidant effects of the Que and TZD derivative administration in adjuvant-induced arthritic (AIA) rats. AIA was induced in Wistar rats by the intraplantar injection of Freund

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Begum, Arifa, Shaheen Begum, Prasad Kvsrg, and Bharathi K. "IN SILICO STUDIES ON FUNCTIONALIZED AZAGLYCINE DERIVATIVES CONTAINING 2, 4-THIAZOLIDINEDIONE SCAFFOLD ON MULTIPLE TARGETS." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 8 (2017): 209. http://dx.doi.org/10.22159/ijpps.2017v9i8.19835.

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Objective: The 2, 4-thiazolidinedione containing compounds could lead to most promising scaffolds with higher efficiency toward the targets recognized for its antidiabetic activity when combined with azaglycine moiety. The objective of the present work was to merge functionalized aza glycines with 2, 4-thiazolidinediones, perform in silico evaluation by molecular properties prediction and undertake the molecular docking studies with targets relevant to diabetes, bacterial and viral infections using Swiss Dock programme for unraveling the target identification which can be used for further desi

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A., N. A. Verdizade K. A. Kuliev K. A. Alieva R. A. Ismailova. "EXTRACTION AND SPECTROPHOTOMETRIC DETERMINATION OF COBALT (II) WITH 3-PHENYL-2, 4-THIAZOLIDINEDIONE." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 11 (2018): 12382–91. https://doi.org/10.5281/zenodo.1490077.

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<em>3-Phenyl<strong>-</strong>2,4- thiazolidinedione (PhTAD) is proposed as an analytical reagent for the extractive spectrophotometric determination of cobalt(II). PhTAD forms blue colored complex with cobalt(II) in the pH range 4.0–5.9. Beer’s law is obeyed in the concentration range up to 16 </em><em>μ</em><em>g mL<sup>−1</sup>. The yellowish Co(II)-PhTAD complex shows a maximum absorbance at 495 nm, with molar absorptivity of 2.62 × 10<sup>4 </sup>dm<sup>3</sup> mol<sup>−1</sup> cm<sup>−1</sup> and Sandell’s sensitivity of the complex obtained f

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Rahman, Safikur, Md Tabish Rehman, Gulam Rabbani, et al. "Insight of the Interaction between 2,4-thiazolidinedione and Human Serum Albumin: A Spectroscopic, Thermodynamic and Molecular Docking Study." International Journal of Molecular Sciences 20, no. 11 (2019): 2727. http://dx.doi.org/10.3390/ijms20112727.

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Thiazolidinedione derivatives (TZDs) have attracted attention because of their pharmacological effects. For example, certain TZDs have been reported to ameliorate type II diabetes by binding and activating PPARs (peroxisome proliferator-activated receptors). Nonetheless, no information is available on the interaction between the heterocyclic 2, 4-thiazolidinedione (2,4-TZD) moiety and serum albumin, which could affect the pharmacokinetics and pharmacodynamics of TZDs. In this study, we investigated the binding of 2,4-TZD to human serum albumin (HSA). Intrinsic fluorescence spectroscopy reveale

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Uwabagira, Nadine, Balladka K. Sarojini, and Ashwini Prabhu. "Synthesis, In Vitro Anticancer, Anti-Inflammatory and DNA Binding Activity of Thiazolidinedione Derivatives." Anti-Cancer Agents in Medicinal Chemistry 20, no. 14 (2020): 1704–13. http://dx.doi.org/10.2174/1871520620666200424102615.

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Background: Cancer is the second leading cause of mortality worldwide. Despite several advances made in the treatment strategies, the cure for cancer remains still a challenge. Currently used treatment modalities pose several side effects and remain ineffective in the later stages. Thiazolidinediones (TZDs) have been shown to possess anti-cancer activity in several in vitro models. Objectives: The objective of this study was to assess the effect of novel synthesized thiazolidinedione derivatives on three selected cancer cell lines viz., human breast adenocarcinoma cell line (MCF-7), lung adeno

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Kyle, Kimberly A., Thomas L. Willett, Laurie L. Baggio, Daniel J. Drucker та Marc D. Grynpas. "Differential Effects of PPAR-γ Activation versus Chemical or Genetic Reduction of DPP-4 Activity on Bone Quality in Mice". Endocrinology 152, № 2 (2010): 457–67. http://dx.doi.org/10.1210/en.2010-1098.

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Abstract Patients with type 2 diabetes mellitus have an increased risk of fracture that can be further exacerbated by thiazolidinediones. A new class of antidiabetic agents control glucose through reduction of dipeptidyl peptidase-4 (DPP-4) activity; however the importance of DPP-4 for the control of bone quality has not been extensively characterized. We compared the effects of the thiazolidinedione pioglitazone and the DPP-4 inhibitor sitagliptin on bone quality in high-fat diet (HFD)-fed wild-type mice. In complementary studies, we examined bone quality in Dpp4+/+ vs. Dpp4−/− mice. Pioglita

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Schwab, A. M., S. Granholm, E. Persson, B. Wilkes, U. H. Lerner, and H. H. Conaway. "Stimulation of Resorption in Cultured Mouse Calvarial Bones by Thiazolidinediones." Endocrinology 146, no. 10 (2005): 4349–61. http://dx.doi.org/10.1210/en.2005-0601.

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Dosage-dependent release of 45Ca was observed from prelabeled mouse calvarial bones after treatment with two thiazolidinediones, troglitazone and ciglitazone. Release of 45Ca by ciglitazone was decreased by the osteoclast inhibitors acetazolamide, calcitonin, 3-amino-1-hydroxypropylidene-1,1-bisphosphonate, and IL-4, but not affected by the peroxisome proliferator-activated receptor γ antagonist, GW 9662, the mitotic inhibitor, hydroxyurea, or indomethacin. Enhanced expression of receptor activator of nuclear factor-κB ligand (RANKL) mRNA and protein and decreased osteoprotegerin (OPG) mRNA an

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Sonawane, L. V., and S. B. Bari. "Synthesis and Spectral Characterization of Some Novel N-Substituted 2, 4-Thiazolidinedione." International Journal of Biological Chemistry 5, no. 1 (2010): 68–74. http://dx.doi.org/10.3923/ijbc.2011.68.74.

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Nastasă, Cristina Mariana, Mihaela Duma, Adrian Pîrnău, Laurian Vlase, Brîndușa Tiperciuc, and Ovidiu Oniga. "Development of new 5-chromenyl-2,4-thiazolidinediones as antimicrobial agents." Medicine and Pharmacy Reports 89, no. 1 (2015): 122–27. http://dx.doi.org/10.15386/cjmed-509.

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Background and aims. In the context of the increasing phenomenon of microbial resistance to usual drugs, the development of new treatment strategies and new therapeutic protocols is a constant need. Thiazolidinedione and chromone represent two important scaffolds in medicinal chemistry due to their large pharmacological applicability.Methods. We synthesized a new 5-(chromene-3-yl)methylene-2,4-thiazolidinedione starting from 6,8-dichloro-4-oxo-4H-chromene-3-carbaldehyde. Then, by treating with different α-bromoalkylarylketones, we obtained N-substituted derivatives. All new compounds were inve

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Munwar, Shaik, K. Ilango, and M. K. Kathiravan. "Synthesis, Molecular Docking Studies and in vitro and in vivo Hypolipidemic Activity of Thiazolidinedione Derivatives." Asian Journal of Chemistry 36, no. 2 (2024): 434–48. http://dx.doi.org/10.14233/ajchem.2024.31107.

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This work aimed to design, synthesize novel thiazolidinedione derivatives, which were tested for their antihyperlipidemic effects. Antihyperlipidemic activity was carried through in silico docking study for the 50 thiazolidinedione derivatives (SMI-IV-1 to 50 derivatives) in comparison with standard pioglitazone against the crystal structure of protein PPARgamma (PDB ID: 6QJ5) proteins. Based on the binding energy further, best three derivatives were selected and characterized with IR, NMR and MASS studies. Then, in vitro evaluation of each derivative's antihyperlipidemic activity was carried

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Ortmeyer, Heidi K., Noni L. Bodkin, Joseph Haney, Shinji Yoshioka, Hiroyoshi Horikoshi, and Barbara C. Hansen. "A Thiazolidinedione ImprovesIn VivoInsulin Action on Skeletal Muscle Glycogen Synthase in Insulin-Resistant Monkeys." International Journal of Experimental Diabetes Research 1, no. 3 (2000): 195–202. http://dx.doi.org/10.1155/edr.2000.195.

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Thiazolidinediones (TZD) have been shown to have anti-diabetic effects including the ability to decrease fasting hyperglycemia and hyperinsulinemia, increase insulin-mediated glucose disposal rate (M) and decrease hepatic glucose production, but the mechanisms of action are not well established. To determine whether a TZD (R-102380, Sankyo Company Ltd., Tokyo, Japan) could improve insulin action on skeletal muscle glycogen synthase (GS), the rate-limiting enzyme in glycogen synthesis, 4 insulin-resistant obese monkeys were given I mg/kg/ day R-102380 p.o. for a 6-week period. Skeletal muscle G

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Anil, Saini, S. Bhatti Ravinder, and S. Sandhu Jagir. "LiBr catalyzed, microwave enhanced synthesis of 5-arylidene rhodanine under solvent free conditions." Journal of Indian Chemical Society Vol. 84, Dec 2007 (2007): 1239–41. https://doi.org/10.5281/zenodo.5825137.

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Department of Chemistry, Punjabi University, Patiala-147 002, Punjab, India <em>E-mail </em>: j_sandhu2002@yahoo.com Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala-147 002, Punjab, India <em>Manuscript received 25 June 2007, accepted 13 September 2007</em> A variety of aldehydes  are condensed with rhodaninc under solvent free conditions using LiBr affording 5-arylidene rhodanines in excellent yields. Also this reaction protocol in extendable to other related systems like pyrazol-5-one and 2,4-thiazolidinedione.

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Nakamura, Shinsuke, Kei Hayashi, Haruka Takizawa, et al. "An Arylidene-Thiazolidinedione Derivative, GPU-4, without PPARγ Activation, Reduces Retinal Neovascularization." Current Neurovascular Research 8, no. 1 (2011): 25–34. http://dx.doi.org/10.2174/156720211794520224.

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Ha, Jeonghoon, Yejee Lim, Mee Kyoung Kim, et al. "Comparison of the Effects of Various Antidiabetic Medication on Bone Mineral Density in Patients with Type 2 Diabetes Mellitus." Endocrinology and Metabolism 36, no. 4 (2021): 895–903. http://dx.doi.org/10.3803/enm.2021.1026.

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Background: Prospective comparative studies on the effects of various antidiabetic agents on bone metabolism are limited. This study aimed to assess changes in bone mass and biochemical bone markers in postmenopausal patients with type 2 diabetes mellitus (T2DM).Methods: This prospective, multicenter, open-label, comparative trial included 264 patients with T2DM. Patients who had received a metformin, or sulfonylurea/metformin combination (Group 1); a thiazolidinedione combination (Group 2); a dipeptidyl peptidase-4 inhibitor (gemigliptin) combination (Group 3); or an sodium-glucose cotranspor

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K., A. Aliyeva. "5- (2-HYDROXYBENZYLIDENE) -2,4-TIAZOLIDINDION AS ANALYTICAL REAGENT FOR EXTRACTION-PHOTOMETRIC DETERMINATION OF COBALT (II)." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES o6, no. 08 (2019): 14980–87. https://doi.org/10.5281/zenodo.3373243.

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<em>The possibility of using 5- (2-hydroxybenzylidene) -2,4-thiazolidinedione (L) for photometric determination of cobalt (II) has been studied. The best extractants were dichloroethane, chloroform and carbon tetrachloride. With a single extraction with chloroform, 97.6% of cobalt is recovered as a complex. The cobalt (II) complex is extracted into chloroform in the pH range 4.0-5.3. The maximum analytical signal for the complexation of cobalt with L is observed at 530 nm. The molar absorption coefficient is 3.28 × 10<sup>4</sup>. The ratio of components in

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Scanlon, James J., and Stephen P. Wren. "Unearthing novel thiazolidinone building blocks as carboxylic acid bioisosteres." Future Medicinal Chemistry 12, no. 20 (2020): 1855–64. http://dx.doi.org/10.4155/fmc-2020-0192.

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Aim: Thiazolidinones were prepared as building blocks for the replacement of carboxylic acids. Materials & methods: Chemical syntheses of thiazolidinones were developed. In addition, the drug-likeness of the target compounds was evaluated in silico. Results: The prepared compounds included the novel structure 4; 5-(3-Iodophenylmethylene)-2,4-thiazolidinedione. Conclusion: Exploration of the methods required to synthesize thiazolidinone building blocks was completed. This work allows future generation of bioisosteric analogs of drugs.

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Schweipert, Markus, Niklas Jänsch, Neha Upadhyay, et al. "Mechanistic Insights into Binding of Ligands with Thiazolidinedione Warhead to Human Histone Deacetylase 4." Pharmaceuticals 14, no. 10 (2021): 1032. http://dx.doi.org/10.3390/ph14101032.

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Recently, we have reported that non-hydroxamate thiazolidinedione (TZD) analogs are capable of inhibiting human deacetylase 4 (HDAC4). This study aims at the dissection of the molecular determinants and kinetics of the molecular recognition of TZD ligands by HDAC4. For this purpose, a structure activity relationship analysis of 225 analogs was combined with a comprehensive study of the enzyme and binding kinetics of a variety of HDAC4 mutant variants. The experimental data were rationalized by docking to the two major conformations of HDAC4. TZD ligands are competitive inhibitors and bind via

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H, Amin Heli, Nileshkumar Joitaram Patel, Patel Nikita, and Patel Dolar Govindbhai. "Investigation of Cardioprotective Effect of 2, 4-thiazolidinedione Derivative Using HFD-STZ Fed Rats." Indian Journal of Pharmaceutical Education and Research 57, no. 1 (2023): 173–81. http://dx.doi.org/10.5530/001954640215.

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Verdizadeh, Nail A., Kerim A. Kuliev, and Konul R. Alieva. "5-(4-hydroxybenzylidene)-2,4-thiazolidinedione as analytical reagents for the extractionphotometric determination of iron(III)." Vestnik Тomskogo gosudarstvennogo universiteta. Khimiya, no. 21 (March 1, 2021): 48–59. http://dx.doi.org/10.17223/24135542/21/5.

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Özlem; AMİRZADEH-KHİABANİ, YILDIRIM. "Alterations of aldose reductase and superoxide dismutase activities by some chromonyl-2, 4-thiazolidinedione derivatives." Ankara Üniversitesi Veteriner Fakültesi Dergisi 61, no. 4 (2014): 249–54. http://dx.doi.org/10.1501/vetfak_0000002638.

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Sunduru, Naresh, Kumkum Srivastava, S. Rajakumar, S. K. Puri, J. K. Saxena, and Prem M. S. Chauhan. "Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials." Bioorganic & Medicinal Chemistry Letters 19, no. 9 (2009): 2570–73. http://dx.doi.org/10.1016/j.bmcl.2009.03.026.

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Abbasi, Fahim, Sang-Ah Chang, James W. Chu, et al. "Improvements in insulin resistance with weight loss, in contrast to rosiglitazone, are not associated with changes in plasma adiponectin or adiponectin multimeric complexes." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 290, no. 1 (2006): R139—R144. http://dx.doi.org/10.1152/ajpregu.00287.2005.

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It has been suggested that changes in adiponectin levels may contribute to improved insulin sensitivity in insulin-resistant individuals both after weight loss and after treatment with thiazolidinedione compounds. If this is correct, then changes in total circulating adiponectin and/or distribution of its multimeric complexes should coincide with improvements in insulin sensitivity after both interventions. To address this issue, fasting adiponectin concentrations and distribution of adiponectin complexes were measured in plasma samples in 24 insulin-resistant, nondiabetic subjects before and

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Eremenko, Tatyana V., Nikolay A. Matsievskiy, Natalya V. Vorokhobina, Irina Y. Matesius, and Irina N. Abramashvili. "Clinical effect of thiazolidinediones in subjects with disorders of carbohydrate metabolism in case of polymorphism rs1801282." Obesity and metabolism 17, no. 2 (2020): 193–99. http://dx.doi.org/10.14341/omet9943.

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BACKGROUND: The polymorphism rs1801282 (Pro12Ala) may be one of the reasons for the heterogeneous response of patients with carbohydrate metabolism disorders to thiazolidinedione therapy. Studies of this polymorphism in patients with metabolic syndrome (MS) will help identify a group of patients in whom the use of thiazolidinedione is advisable. AIMS: To assess the clinical effect of thiazolidinediones in patients with metabolic syndrome, depending on the presence of polymorphism rs1801282. MATERIALS AND METHODS: All patients with newly diagnosed MS with impaired carbohydrate metab

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Shukla, Karuna S., Shailendra Pandey, and Pooja Chawla. "Synthesis of Some 5-(substituted benzylidene-2, 4-dioxothiazolidin-3-yl) benzoic Acid Derivatives by Conventional and Microwave-assisted Methods and Evaluation of their Potential as Antimicrobial Agents." Anti-Infective Agents 17, no. 2 (2019): 115–29. http://dx.doi.org/10.2174/2211352516666181024151213.

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<P>Background: Multiple antibiotic resistant bacteria represent a challenge in the treatment of infections. It is imperative, therefore, that new substances with antimicrobial properties should be searched to fight these microorganisms. Objective: A series of 5-benzylidene-2, 4-dioxothiazolidin-3-yl benzoic acid derivatives were synthesized and evaluated their antimicrobial potential. The compounds were synthesized by both conventional and microwave synthesizers. Methods: In this study, a series of 5-benzylidene-2, 4-dioxothiazolidin-3-yl benzoic acid derivatives were synthesized by Knoe

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Kim, Kyongyoung. "Anti-Diabetic Medications and Osteoporosis." Journal of Korean Diabetes 24, no. 4 (2023): 173–77. http://dx.doi.org/10.4093/jkd.2023.24.4.173.

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Osteoporosis and diabetes mellitus are chronic diseases that are rapidly increasing in our aging society.Several studies have reported that the incidence of osteoporosis and fractures is increased in diabeticpatients. Although diabetes itself can affect bone density, anti-diabetic medications can also cause changesin bone mineral density, leading to osteoporosis. It is well known that thiazolidinedione increases the riskof fracture. In comparison, metformin, dipeptidyl peptidase-4 inhibitors, sodium glucose cotransporter2 inhibitors, and glucagon-like peptide-1 receptor agonists have no signif

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Barbosa, Karla P. S., Laise A. M. Santos, Edlene L. Ribeiro, et al. "Reduction of carrageenan-induced acute pulmonary inflammation in mice by novel thiazolidinedione derivative LPSF/RA-4." European Journal of Pharmacology 718, no. 1-3 (2013): 197–205. http://dx.doi.org/10.1016/j.ejphar.2013.08.033.

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Nadia, Aida, Antonius Herry Cahyana, Dicky Annas, Mohammad Jihad Madiabu, and Bayu Ardiansah. "Green catalyst of cobalt ferrite magnetic nanoparticles using petai peel extract for the synthesis of thiazolidinedione-based chalcone 4H-thiopyran as an antioxidant." RSC Advances 14, no. 34 (2024): 24384–97. http://dx.doi.org/10.1039/d4ra03077j.

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Kim, Won Jun, Jung Hyun Noh, Kyungdo Han, and Cheol-Young Park. "The Association Between Second-Line Oral Antihyperglycemic Medication on Types of Dementia in Type 2 Diabetes: A Nationwide Real-World Longitudinal Study." Journal of Alzheimer's Disease 81, no. 3 (2021): 1263–72. http://dx.doi.org/10.3233/jad-201535.

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Background: There are few reports that evaluated the association between various types of dementia and dual oral therapy with antihyperglycemic medication. Objective: The goal of this study was to investigate the association between treatment of dual antihyperglycemic medication and dementia subclass in type 2 diabetes mellitus using the Korean National Health Insurance System. Methods: This study included 701,193 individuals with diabetes prescribed dual oral therapy between 2009 and 2012 from the Korean National Health Insurance Service Database, which were tracked until 2017. All-cause, Alz

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Phillips, Susan A., Theodore P. Ciaraldi, Deborah K. Oh, Michelle K. Savu, and Robert R. Henry. "Adiponectin secretion and response to pioglitazone is depot dependent in cultured human adipose tissue." American Journal of Physiology-Endocrinology and Metabolism 295, no. 4 (2008): E842—E850. http://dx.doi.org/10.1152/ajpendo.90359.2008.

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The subcutaneous (S) and visceral (V) adipose tissue (AT) depots are increasingly recognized as distinct. To test the hypothesis that depot differences exist for adiponectin, fresh and cultured human VAT and SAT from obese type 2 diabetic (T2D) and obese nondiabetic (ND) subjects was examined to determine whether differences in adiponectin content and secretion occurred as a function of depot studied, diabetic status, and response to thiazolidinedione treatment. VAT and SAT were obtained by biopsy and AT explants cultured in defined media for 7 days. Protein expression was assessed by Western

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Moon, Kyoung-Sik, Jung-Ho Noh, Yong-Bum Kim, et al. "Subacute toxicity study of CKD-501, a novel thiazolidinedione, after 4-week repeated oral administration in mice." Toxicology Letters 221 (August 2013): S255. http://dx.doi.org/10.1016/j.toxlet.2013.05.637.

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Cabré, A., I. Lázaro, J. Girona, et al. "Fatty acid binding protein 4 is increased in metabolic syndrome and with thiazolidinedione treatment in diabetic patients." Atherosclerosis 195, no. 1 (2007): e150-e158. http://dx.doi.org/10.1016/j.atherosclerosis.2007.04.045.

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Arima, Shuji, Kentaro Kohagura, Kazuhisa Takeuchi, et al. "Biphasic Vasodilator Action of Troglitazone on the Renal Microcirculation." Journal of the American Society of Nephrology 13, no. 2 (2002): 342–49. http://dx.doi.org/10.1681/asn.v132342.

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ABSTRACT. Recent studies have demonstrated that thiazolidinediones, novel antidiabetic compounds that improve the insulin sensitivity, lower BP and decrease urinary protein excretion. However, neither the target vasculature nor the underlying mechanism for their actions is well understood. In this study, the action of troglitazone (Tro), a thiazolidinedione compound, on the glomerular afferent (Af-Arts) and efferent (Ef-Arts) arterioles, crucial vascular segments to the control of glomerular hemodynamics, were directly examined. Rabbit Af-Arts or Ef-Arts were microdissected from the superficia

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Froes, Thamires Quadros, Rafael VC Guido, Kamel Metwally, and Marcelo Santos Castilho. "A novel scaffold to fight Pseudomonas aeruginosa pyocyanin production: early steps to novel antivirulence drugs." Future Medicinal Chemistry 12, no. 16 (2020): 1489–503. http://dx.doi.org/10.4155/fmc-2019-0351.

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Aim: Although bacterial resistance is a growing concern worldwide, the development of antibacterial drugs has been steadily decreasing. One alternative to fight this issue relies on reducing the bacteria virulence without killing it. PhzS plays a pivotal role in pyocyanin production in Pseudomonas aeruginosa. Results: A total of 31 thiazolidinedione derivatives were evaluated as putative PhzS inhibitors, using thermo shift assays. Compounds that significantly shifted PhzS's Tm had their mode of inhibition (cofactor competitor) and affinity calculated by thermo shift assays as well. The most pr

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Lee, Sang Ah, Young Ree Kim, Eun Jin Yang, et al. "CD26/DPP4 Levels in Peripheral Blood and T Cells in Patients With Type 2 Diabetes Mellitus." Journal of Clinical Endocrinology & Metabolism 98, no. 6 (2013): 2553–61. http://dx.doi.org/10.1210/jc.2012-4288.

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Context: Dipeptidyl peptidase 4 (CD26/DPP4) is expressed on blood T cells and also circulates in a soluble form (sCD26/DPP4). Objective: We aimed to evaluate blood T cell and circulating CD26/DPP4 and its association with metabolic parameters in patients with type 2 diabetes mellitus (T2DM). Designs: We measured CD26/DPP4 expression (percentage of CD26+ cells using flow cytometry) on CD4+ and CD8+ T cells, serum CD26/DPP4 level and activity, and various metabolic parameters in T2DM patients not on DPP4 inhibitor therapy (n = 148). Nondiabetic subjects (n = 50) were included as a control group.

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Lgaz, Hassane, Sourav Kr Saha, Han-seung Lee, et al. "Corrosion Inhibition Properties of Thiazolidinedione Derivatives for Copper in 3.5 wt.% NaCl Medium." Metals 11, no. 11 (2021): 1861. http://dx.doi.org/10.3390/met11111861.

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Copper is the third-most-produced metal globally due to its exceptional mechanical and thermal properties, among others. However, it suffers serious dissolution issues when exposed to corrosive mediums. Herein, two thiazolidinedione derivatives, namely, (Z)-5-(4-methylbenzylidene)thiazolidine-2,4-dione (MTZD) and (Z)-3-allyl-5-(4-methylbenzylidene)thiazolidine-2,4-dione (ATZD), were synthesized and applied for corrosion protection of copper in 3.5 wt.% NaCl medium. The corrosion inhibition performance of tested compounds was evaluated at different experimental conditions using electrochemical

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Sameeh, Manal Y., Manal M. Khowdiary, Hisham S. Nassar, et al. "Thiazolidinedione Derivatives: In Silico, In Vitro, In Vivo, Antioxidant and Anti-Diabetic Evaluation." Molecules 27, no. 3 (2022): 830. http://dx.doi.org/10.3390/molecules27030830.

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This work aimed to synthesize a new antihyperglycemic thiazolidinedione based on the spectral data. The DFT\B3LYP\6-311G** level of theory was used to investigate the frontier molecular orbitals (FMOs), chemical reactivity and map the molecular electrostatic potentials (MEPs) to explain how the synthesized compounds interacted with the receptor. The molecular docking simulations into the active sites of PPAR-γ and α-amylase were performed. The in vitro potency of these compounds via α-amylase and radical scavenging were evaluated. The data revealed that compounds (4–6) have higher potency than

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Somayajulu, D. L. N., A. V. L. N. S. H. Hariharan, and Y. Subhash. "Solvent free synthesis of active 5-benzylidine-1, 3-thiazolidine-2,4-dione derivatives." Research Journal of Chemistry and Environment 25, no. 12 (2021): 68–71. http://dx.doi.org/10.25303/2512rjce6871.

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Present communication describes the attempts made to improve the yields of thiazolidinedione group of derivatives keeping in view of their anti-cancer activity. 5-benzylidine-1,3-thiazolidine-2,4-dione derivatives were the active substrates belonging to α-glucosidase inhibitor classification. These were prepared by the reaction of 4-((Z)-(2,4-dioxothiazolidin-5-ylidene) methyl) benzaldehyde with aromatic/hetero aromatic ketones in the presence of potassium hydroxide and ethanol as solvent. Synthesis of 5-benzylidine-1, 3-thiazolidine-2,4-dione derivatives has been optimized under solvent free

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Haigh, David, Helen C. Birrell, Barrie C. C. Cantello, et al. "Non-thiazolidinedione antihyperglycaemic agents. Part 4: Synthesis of (±)-, (R)-(+)- and (S)-(−)-enantiomers of 2-oxy-3-arylpropanoic acids." Tetrahedron: Asymmetry 10, no. 7 (1999): 1335–51. http://dx.doi.org/10.1016/s0957-4166(99)00104-4.

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Voskoboinikova, Halyna L., Yevhenii P. Bohuslavskyi, Victoria V. Dovzhuk, Liudmyla V. Konovalova, and Natela Sh Dovzhuk. "ASPECTS OF THE USE OF ANTIDIABETIC DRUGS IN PHARMACEUTICAL PRACTICE ON THE BASIS OF RATIONAL PHARMACOTHERAPY." Клінічна та профілактична медицина, no. 3 (May 8, 2024): 13–20. http://dx.doi.org/10.31612/2616-4868.3.2024.02.

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The aim of the article. To study of the incidence of diabetes mellitus in Ukraine and to determine the prospects for the use and pharmaceutical development of antidiabetic drugs. Materials and methods. Data from the State Registers of Medicinal Products of Ukraine, of Wholesale and Retail Prices for Medicinal Products declared in Ukraine under an international non-proprietary or generic name (01.01.2024). Were used: systematic and comparative analysis, processing and synthesis, and generalization to determine the forecasted prospects. Results. In Ukraine the number of diabetes patients increas

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Lelyukh, Maryan, Myroslava Kalytovska, Marta Zastryzhna, Arkadii Savchenko, Ihor Chaban, and Stefan Harkov. "Synthesis and antitumor activity of 1,3,4-oxadiazole substituted 2-(5-ylidene-2,4-dioxothiazolidin-3-yl)-acetamides." Pharmacia 70, no. (4) (2023): 1093–100. https://doi.org/10.3897/pharmacia.70.e102449.

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A series of novel 1,3,4-oxadiazole substituted 2-(5-aryl/heterylidene-2,4-dioxothiazolidine-3-ylidene)-acetamides and their 5-unsubstituted analogues have been synthesized following <i>N</i>-alkylation reaction of 2-chloro-<i>N</i>-(5-aryl-[1,3,4]oxadiazol-2-yl)-acetamides with thiazolidinedione and potassium salts of its arylidene derivatives. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. Evaluation of anticancer activity <i>in vitro</i> for the synthesized compounds was performed in accordance with the National Cancer Institute protoco

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