Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. Their solubility in alcohol is lower than that in water and decreases with increasing molecular weight of the alcohols . Application of C4H6N2S.
Li, Zhonghua;Qin, Tingting;Li, Zhongrui;Zhao, Xuan;Zhang, Xinhui;Zhao, Taoqian;Yang, Nian;Miao, Jinxin;Ma, Jinlian;Zhang, Zhenqiang research published 《 Discovery of quinazoline derivatives as a novel class of potent and in vivo efficacious LSD1 inhibitors by drug repurposing》, the research content is summarized as follows. Histone lysine-specific demethylase 1 (LSD1) is an important epigenetic modulator, and is implicated in malignant transformation and tumor pathogenesis in different ways. Therefore, the inhibition of LSD1 provides an attractive therapeutic target for cancer therapy. Based on drug repurposing strategy, we screened our inhouse chem. library toward LSD1, and found that the EGFR inhibitor erlotinib, an FDA-approved drug for lung cancer, possessed low potency against LSD1 (IC50 = 35.80 μM). Herein, we report our further medicinal chem. effort to obtain a highly water-soluble erlotinib analog 5k (>100 mg/mL) with significantly enhanced inhibitory activity against LSD1 (IC50 = 0.69 μM) as well as higher specificity. In MGC-803 cells, 5k suppressed the demethylation of LSD1, indicating its cellular activity against the enzyme. In addition, 5k had a remarkable capacity to inhibit colony formation, suppress migration and induce apoptosis of MGC803 cells. Furthermore, in MGC-803 xenograft mouse model, 5k treatment resulted in significant reduction in tumor size by 81.6% and 96.1% at dosages of 40 and 80 mg/kg/d, resp. Our findings indicate that erlotinib-based analogs provide a novel structural set of LSD1 inhibitors with potential for further investigation, and may serve as novel candidates for the treatment of LSD1-overexpressing cancers.
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