Category: 884494-45-5

Rong, Jian published the artcileNovel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine, the main research area is piperazinyl azetidine PET ligand preparation imaging monoacylglycerol lipase.

Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system. Inhibition of MAGL constitutes an attractive therapeutic concept for treating psychiatric disorders and neurodegenerative diseases. Herein, we present the design and synthesis of multiple reversible MAGL inhibitor candidates based on a piperazinyl azetidine scaffold. Compounds 10 and 15 were identified as the best-performing reversible MAGL inhibitors by pharmacol. evaluations, thus channeling their radiolabeling with fluorine-18 in high radiochem. yields and favorable molar activity. Furthermore, evaluation of [18F]10 and [18F]15 ([18F]MAGL-2102) by autoradiog. and positron emission tomog. (PET) imaging in rodents and nonhuman primates demonstrated favorable brain uptakes, heterogeneous radioactivity distribution, good specific binding, and adequate brain kinetics, and [18F]15 demonstrated a better performance. In conclusion, [18F]15 was found to be a suitable PET radioligand for the visualization of MAGL, harboring potential for the successful translation into humans.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Ren, Li published the artcileDiscovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2, Safety of 2-Fluoro-4-iodo-6-methylpyridine, the main research area is pyridone ERK inhibitor pharmacokinetics.

Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of I, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, I was selected for further preclin. evaluation.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Safety of 2-Fluoro-4-iodo-6-methylpyridine.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Montgomery, Justin I. published the artcilePyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections, Formula: C6H5FIN, the main research area is pyridone methylsulfone hydroxamate LpxC inhibitor treatment gram neg infection.

The synthesis and biol. activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a (I) is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-neg. antibacterial activity to comparator agents.

Journal of Medicinal Chemistry published new progress about Acinetobacter. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Formula: C6H5FIN.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com