Development of N-[4-[6-(Isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[11C]methylbenzamide for Positron Emission Tomography Imaging of Metabotropic Glutamate 1 Receptor in Monkey Brain was written by Fujinaga, Masayuki;Yamasaki, Tomoteru;Maeda, Jun;Yui, Joji;Xie, Lin;Nagai, Yuji;Nengaki, Nobuki;Hatori, Akiko;Kumata, Katsushi;Kawamura, Kazunori;Zhang, Ming-Rong. And the article was included in Journal of Medicinal Chemistry in 2012.COA of Formula: C8H7ClN4S The following contents are mentioned in the article:
Three novel 4-substituted benzamides have been synthesized as potential ligands for the positron emission tomog. (PET) imaging of metabotropic glutamate 1 (mGlu1) receptor in the brain. Of these compounds, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-N,4-dimethylbenzamide (4) exhibited the highest binding affinity (Ki = 13.6 nM) for mGlu1 and was subsequently labeled with carbon-11. In vitro autoradiog. using rat brain sections showed that [11C]4 binding was consistent with the distribution of mGlu1, with high specific binding in the cerebellum and thalamus. PET studies with [11C]4 in monkey showed a high brain uptake and a kinetic profile suitable for quant. anal. Pretreatment with a mGlu1-selective ligand 16 largely decreased the brain uptake, indicating high in vivo specific binding of [11C]4 to mGlu1. In metabolite anal., only unchanged [11C]4 was found in the brain. [11C]4 is a useful PET ligand for the imaging and quant. anal. of mGlu1 in monkey brain and merits further evaluation in humans. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2COA of Formula: C8H7ClN4S).
4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.COA of Formula: C8H7ClN4S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica