A series of compounds was synthesized by linking various derivatives of pyridine, pyrimidine or pyrazine to thiazole-2-thiol or to its partially hydrogenated derivative 2-thiazoline-2-thiol. The reactions of the compounds with molecular iodine and lactoperoxidase were examined in vitro. Their antithyroid activity was also examined in vivo in the rat. T4 and TSH levels were determined, and the thyroid gland was examined histologically. 2-(3-Hydroxy-2-pyridyl)-2-thiothiazoline had the highest antithyroid activity of the compounds tested (Kc = 14931.mol(-1),IC(50)0.65 x 10(-4) M, activity of thyroid gland).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/cpb.41.1258 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Anti-cancer effect of midazolam via downregulating YWHAH in papillary thyroid cancer cells.
Discov Oncol
January 2025
Department of Anesthesiology, The First Affiliated Hospital, Zhejiang University School of Medicine, No.1367 Wenyi West Road, Yuhang District, Hangzhou, 311100, People's Republic of China.
The work is aimed to investigate whether midazolam functions in thyroid cancer and reveal the potential mechanism of action. Cell viability was detected by CCK-8 method when treated by varying doses of midazolam to detect the cytotoxicity of midazolam on human thyroid follicular epithelial cell line and thyroid cancer cell lines. In thyroid cancer cells, EDU staining, wound healing and transwell assays were respectively used to detect cell proliferation, migration and invasion.
View Article and Find Full Text PDFAutoimmune Polyglandular Syndrome Type 3: A Case Report.
Cureus
December 2024
Internal Medicine, Centro Hospitalar de Trás-os-Montes e Alto Douro, Vila Real, PRT.
Autoimmune polyglandular syndromes (APS) are characterized by associations of two or more autoimmune diseases (AID). APS type 3 is characterized by the presence of autoimmune thyroid disease associated with other AID, excluding adrenal gland involvement. Here we report a case of a 64-year-old male, with history of type 1 diabetes mellitus (T1DM), diagnosed at the age of 32, who was referred to a Diabetes consultation in 2014 due to poor metabolic control.
View Article and Find Full Text PDFLittle is known about the impact of environmental pollution on thyroid function in the non-occupationally exposed population of Kazakhstan. This study aimed to investigate serum levels of thyroxine (T4), thyroid-stimulating hormone (TSH), and anti-thyroid peroxidase (TPO) antibodies in the environmentally exposed population of Kazakhstan in relation to symptoms of anxiety. A total of 1,388 nominally healthy individuals residing in areas exposed to three major types of environmental pollution prevalent in Kazakhstan-non-ferrous metallurgy, condensate gas extraction, and activities of the Semipalatinsk Nuclear Test Site (SNTS)-were enrolled.
View Article and Find Full Text PDFTreatment of Hyperthyroidism in Graves' Disease Complicated by Thyroid Eye Disease.
J Clin Endocrinol Metab
January 2025
Department of Ophthalmology and Visual Sciences and Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48105 USA.
Thyroid eye disease (TED) is the most consequential extrathyroidal manifestation or complication of Graves' disease (GD). Treatment of hyperthyroidism in GD complicated by TED is challenging. Antithyroid drugs (ATDs) and thyroidectomy do not change the natural course of TED, while radioactive iodine (RAI) is associated with a small but well-documented risk of TED de novo occurrence or its progression/worsening.
View Article and Find Full Text PDFElimination of oral foci of infection might lead to clinical improvement of Graves' orbitopathy.
Graefes Arch Clin Exp Ophthalmol
January 2025
Department of Endocrinology, Metabolism and Internal Medicine, Poznan University of Medical Sciences, Przybyszewskiego 49, 60-355, Poznan, Poland.
Purpose: Graves' disease (GD) and Graves' orbitopathy (GO) are multifactorial disorders with links to the gut microbiome and autoimmunity. It is observed that patients with GD exhibit altered gut microbiome diversity. However, little is known about the role of oral microbiota in GD and GO.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!