Synthesis and Evaluation of 3,4-Dihydropyrimidin-2(1H)-ones as Sodium Iodide Symporter Inhibitors was written by Lacotte, Pierre;Puente, Celine;Ambroise, Yves. And the article was included in ChemMedChem in 2013.Product Details of 1122-71-0 This article mentions the following:
The sodium iodide symporter (NIS) is responsible for the accumulation of iodide in the thyroid gland. This transport process is involved in numerous thyroid dysfunction and is the basis for human contamination in the case of exposure to radioactive iodine species. 4-Aryl-3,4-dihydro-2(1H)-pyrimidinone derivatives were recently discovered by high-throughput screening as the first NIS inhibitors. Described herein are the synthesis and evaluation of 115 derivatives with structural modifications at five key positions on the pyrimidone core. This study provides extensive structure-activity relationships for this new class of inhibitors that will serve as a basis for further development of compounds with in vivo efficacy and adequate pharmacokinetic properties. In addition, the SAR investigation provided a more potent compound, which exhibits an IC50 value of 3.2 n in a thyroid cell line (FRTL5, animal model, rat model). The title compounds thus formed included analogs and derivatives of 1,2,3,4-tetrahydro-6-methyl-2-oxo-4-phenyl-5-pyrimidinecarboxylic acid (4-methoxyphenyl)methyl ester (I), such as thiophene derivatives, pyridine derivatives, imidazole derivatives, naphthalene derivatives, etc. The synthesis of the target compounds was achieved using Meldrum’s acid, amines aldehydes and alcs. as simple starting materials. In the experiment, the researchers used many compounds, for example, 6-Methyl-2-pyridinemethanol (cas: 1122-71-0Product Details of 1122-71-0).
6-Methyl-2-pyridinemethanol (cas: 1122-71-0) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Product Details of 1122-71-0
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts