Academic literature on the topic '4-thiazolidinedione'

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Journal articles on the topic "4-thiazolidinedione"

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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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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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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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Dissertations / Theses on the topic "4-thiazolidinedione"

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Kyle, Kimberly Anne. "Differential Effects of PPAR-γ Activation vs. Chemical or Genetic Reduction of DPP-4 Activity on Murine Bone Quality". Thesis, 2010. http://hdl.handle.net/1807/25738.

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This study characterized the effects of two anti-diabetic drugs, a thiazolidinedione (TZD) and a Dipeptidyl Peptidase-4 (DPP-4) inhibitor on bone quality in a glucose intolerant mouse model. Bone quality in a DPP-4 -/- mouse model was also examined. Bone quality was evaluated through densitometry, mechanical testing and techniques to assess remodeling, structural and mineral properties. TZD treatment negatively affected trabecular mechanical properties in male, female and ovariectomized female (OVX) mice. Male mice exhibited the greatest effect due to TZD treatment with reduced vertebral vBMD,
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Book chapters on the topic "4-thiazolidinedione"

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Ranjbar, Tara, Jennifer L. O’Connor, and Khosrow Kashfi. "Therapeutic Management of Type 2 Diabetes: The Nitric Oxide Axis." In The Role of Nitric Oxide in Type 2 Diabetes. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815079814122010013.

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According to the World Health Organization (WHO), the prevalence of obesity across the globe has nearly tripled since 1975, with 39 million children under the age of 5 being overweight or obese in 2020. Obesity is the most common risk factor for developing type 2diabetes (T2D), which may lead to elevated serum triglycerides, hypertension, and insulin resistance. In the pathogenesis of T2D, there is a reduction in nitric oxide (NO) bioavailability. Restoration of NO levels has been associated with many favorable metabolic effects in T2D. Drugs that potentiate NO levels may have a role in improv
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Islam, Mr Mohidul, Ms Jayashree Devi, Mr Josef Yakin, and Mr Mukinur Hussain. "Anti-diabetic Activity: Methods for Evaluation." In Pharmaceutical Science: Research and Innovation. Iterative International Publishers, Selfypage Developers Pvt Ltd, 2024. http://dx.doi.org/10.58532/psrich14.

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Diabetes mellitus is a chronic condition characterized by insufficient insulin production or ineffective insulin utilization, resulting in elevated blood glucose levels. This review outlines the various types of diabetes, including type 1, type 2, and gestational diabetes, and their potential complications, such as cardiovascular diseases, neuropathy, and nephropathy. It explores the mechanisms of action and examples of common anti-diabetic medications, including biguanides, sulfonylureas, meglitinides, thiazolidinediones, alpha-glucosidase inhibitors, DPP-4 inhibitors, and SGLT2 inhibitors. T
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Bailey, Clifford J., and Melanie J. Davies. "Non-Insulin Glucose-Lowering Agents." In Oxford Textbook of Endocrinology and Diabetes 3e, edited by John A. H. Wass, Wiebke Arlt, and Robert K. Semple. Oxford University Press, 2021. http://dx.doi.org/10.1093/med/9780198870197.003.0253.

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A selection of differently acting blood glucose-lowering agents can be used in the management of type 2 diabetes to address different aspects of disease pathogenesis and comorbidities. Key factors influencing choice of medication include extent and duration of hyperglycaemia, obesity, insulin resistance, and impairment of beta-cell function, risk of hypoglycaemia, and risk or presence of cardiovascular, renal, and other complications. Diet, other lifestyle measures, patient education, and empowerment are fundamental throughout. Metformin is still widely used as initial orally administered bloo
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Sarfraz, Maliha, Rahman M. Hafizur, Hayat Ullah, et al. "Current Strategies of New Drugs for Diabetes Management." In Frontiers in Clinical Drug Research-Diabetes and Obesity: Volume 7. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815123586123070005.

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Several aspects need to be explored in drug therapy for diabetes patients. Some specific glucose-reducing medicines are present, while other medicines are associated with unintentional changes in hyperglycemia. Diabetes is a developing epidemic that has caused significant socioeconomic problems in several countries throughout the world. Despite scientific discoveries, greater healthcare services, and higher literacy rates, the disease continues to plague many industries, particularly developing countries. The current trends show an increase in premature mortality, which threatens world prosper
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Faruk Khan, M. O. "Diabetes and Antidiabetic Drugs." In Medicinal Chemistry for Pharmacy Students. BENTHAM SCIENCE PUBLISHERS, 2024. http://dx.doi.org/10.2174/9789815179729124030009.

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This chapter is a comprehensive account of diabetes and the medicinal chemistry of antidiabetic drugs. It provides the mechanism of disease progression and drug action and detailed structure-activity relationships (SAR) of antidiabetic drugs to give the knowledge base for pharmacists. After studying this chapter, students will be able to: • Discuss the epidemiology and etiology of diabetes. • Describe the clinical features of diabetes and differentiate between type I and type II diabetes. • Discuss various risk factors and corresponding mechanisms responsible for the development of diabetes. R
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Conference papers on the topic "4-thiazolidinedione"

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Zaghloul, Nancy, Ahmed Awaisu, Ahmed Mahfouz, Sumaya Al Saadi, and Hazem Elewa. "Trends of use of SGLT2 inhibitors in Qatar." In Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2021. http://dx.doi.org/10.29117/quarfe.2021.0108.

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Background: Type 2 diabetes mellitus (T2DM) represents a growing health challenge in Qatar and worldwide. T2DM is associated with a high risk of cardiovascular (CV) morbidity and mortality, and progression of renal disease. Sodium glucose co-transporter 2 inhibitors (SGLT2is) are the most recently approved class of glucose lowering medications (GLMs). To date, there is a limited knowledge about the adoption of SGLT2is by clinicians compared to other oral GLMs in Qatar and Middle East and North Africa (MENA) region. Accordingly, this proposed study aims to explore the trends in SGLT2is use comp
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