methimazole

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

Methimazole D3, a deuterium-labeled version of Methimazole, serves as an antithyroid medication for treating hyperthyroidism in both humans and animals.

1-Methylimidazole is a metabolite of 1-methyl-2-thioimidazole (methimazole) which inhibits bone resorption.

Carbimazole (Athyromazole) is an Imidazolium thyroid antagonist, which is rapidly transformed into MMI in vivo and can be converted into methidazole in vitro, and can be used in the study of Graves' disease.

1-Methyl-2-(methylthio)imidazole is an impurity of Methimazole and a thiourea antithyroid agent.

TG-100435 is a novel multi-target oral protein tyrosine kinase inhibitor. The metabolic flux of TG100435 is entirely inhibited by methimazole and ketoconazole. In human liver microsomes or recombinant P450, the formation of TG100435 increases with the activity of cytochrome P450 reductase, suggesting that cytochrome P450 reductase may be involved.

The leguminous shrub,Leucaena leucocephala(Leucaena) is wide‐spread in tropical and subtropical agricultural systems and provides a ready source of protein for livestock. However, the presence of mimosine, a non‐protein, amino acid comprising about 12% of the dry matter in growing tips ofLeucaena, is toxic to animals. Mimosine is degraded rapidly in the rumen to produce 3,4‐dihydroxypyridine (3,4‐DHP) and 2,3‐dihydroxypyridine (2,3‐DHP), both of which remain toxic to animals[1]. 3,4-DHP, as a derivative of the plant amino acid mimosine, is goitrogenic in cattle, sheep, and mice. In contrast to established antithyroid compounds, such as methimazole (MMI) and propylthiouracil (PTU), 3,4-DHP has no SH-group. 3,4-DHP with various concentrations inhibited incorporation of125I into protein in human thyroid slices. It also suppressed the activation of lymphocytes by PHA (phytohaemagglutinin) and PWM (pokeweed mitogen). Suppression with 3,4-DHP was seen at 100 and 1000 μmol L (P< 0.001 vs both PHA and PWM). Those, together with a very low murine bone marrow toxicity, probably related to the absence of an SH-group, make 3,4-DHP a potential antithyroid drug[2].