Imidazole based anticancer drug find applications in cancer chemotherapy. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). Application of C4H6N2S.
Trzos, Sara;Link-Lenczowski, Pawel;Sokolowski, Grzegorz;Pochec, Ewa research published 《 Changes of IgG N-glycosylation in thyroid autoimmunity: the modulatory effect of methimazole in graves’ disease and the association with the severity of inflammation in Hashimoto’s thyroiditis》, the research content is summarized as follows. The N-glycome of IgG (IgG), the most abundant glycoprotein in human blood serum, reflects pathol. conditions of autoimmunity and is sensitive to medicines applied in disease therapy. Due to the high sensitivity of N-glycosylation, the IgG N-glycan profile may serve as an indicator of an ongoing inflammatory process. The IgG structure and its effector functions are strongly dependent on the composition of Nglycans attached to the Fc fragment, and the binding of antigens is regulated by Fab sugar moieties. Because of the crucial role of N-glycans in IgG function, remodeling of its Noligosaccharides can induce pathol. changes that ultimately contribute to the development of autoimmunity; restoration of their physiol. structure is critical to the reduction of disease symptoms. Our recently published data have shown that the pathol. of autoimmune thyroid diseases (AITDs), including Hashimoto’s thyroiditis (HT) and Graves’ disease (GD), is accompanied by alterations of the composition of IgG Nglycans. The present study is a more in-depth investigation of IgG glycosylation in both AITDs, designed to determine the relationship between the severity of thyroid inflammation and IgG N-glycan structures in HT, and to assess the impact of immunosuppressive therapy on the N-glycan profile in GD patients. The study material consisted of human serum samples collected from donors with elevated anti-thyroglobulin (Tg) and/or anti-thyroperoxidase (TPO) IgGs without symptoms of hypothyroidism (n=68), HT patients characterized by high autoantibody titers and advanced destruction of the thyroid gland (n=113), GD patients with up-regulated IgG against TSH receptor (TSHR) before (n=62) and after (n=47) stabilization of TSH level as a result of methimazole therapy (study groups), and healthy donors (control group, n=90). IgG was isolated from blood serum using protein G affinity chromatog. N-glycans were released from IgG by PNGase F digestion and analyzed by ultra-performance liquid chromatog.-mass spectrometry (UPLC-MS) after 2-aminobenzamide (2-AB) labeling. UPLC-MS chromatograms were integrated into 25 peaks (GP) in the Waters UNIFI Scientific Information System, and N-glycans were assigned based on the glucose unit values and mass-to-charge ratios (m/z) of the detected ions. The Kruskal-Wallis nonparametric test was used to determine the statistical significance of the results (p<0.05). The obtained results suggest that modifications of IgG sialylation, galactosylation and core-fucosylation are associated with the severity of HT symptoms. Methimazole therapy implemented in GD patients affected the IgG N-glycan profile; as a result, the content of the sialylated and galactosylated oligosaccharides with core fucose differed after treatment. Our results suggest that N-glycosylation of IgG undergoes dynamic changes during the intensification of thyroiditis in HT, and that in GD autoimmunity it is affected significantly by immunosuppressive therapy.
60-56-0, Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.
Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.
Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.
Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.
Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).
Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., Application of C4H6N2S
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem