Synthesis and Evaluation of 4-Halogeno-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-[11C]methylbenzamide for Imaging of Metabotropic Glutamate 1 Receptor in Melanoma was written by Fujinaga, Masayuki;Xie, Lin;Yamasaki, Tomoteru;Yui, Joji;Shimoda, Yoko;Hatori, Akiko;Kumata, Katsushi;Zhang, Yiding;Nengaki, Nobuki;Kawamura, Kazunori;Zhang, Ming-Rong. And the article was included in Journal of Medicinal Chemistry in 2015.Category: thiazole The following contents are mentioned in the article:
Isopropylaminopyrimidinylthiazolyl halobenzamides I (R = H, Me; R1 = Cl, Br, I) were prepared as inhibitors of metabotropic glutamate 1 (mGlu1) receptors for potential use in the treatment of melanoma; I (R = 11CH3; R1 = Cl, Br, I) were prepared and tested as PET imaging agents for mGlu1-containing melanomas with decreased affinities for concentration in brain tissue. I (R = Me; R1 = Cl, Br, I) bound to mGlu1 with Ki values of 22-143 nM. In vivo biodistribution studies of I (R = 11CH3; R1 = Cl, Br, I) in mice implanted with B16F10 melanoma cells confirmed high radioactive uptake in tumor and low uptake in blood, skin, and muscles; inhibition of mGlu1 receptor using an mGlu1-selective ligand led to reduced radioactive uptake in the tumor. I (R = 11CH3; R1 = I) displayed the highest ratio of uptake between tumor and nontarget tissue and may prove useful as a PET tracer for mGlu1 imaging in melanoma. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2Category: thiazole).
4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica