Taylor, Steven J.; Abeywardane, Asitha; Liang, Shuang; Xiong, Zhaoming; Proudfoot, John R.; Farmer, Bennett Sandy; Gao, Donghong A.; Heim-Riether, Alexander; Smith-Keenan, Lana Louise; Muegge, Ingo; Yu, Yang; Zhang, Qiang; Souza, Donald; Panzenbeck, Mark; Goldberg, Daniel; Hill-Drzewi, Melissa; Margarit, Mariana; Collins, Brandon; Li, John Xiang; Zuvela-Jelaska, Ljiljana; Li, Jun; Farrow, Neil A. published an article in 2021. The article was titled 《Indole Inhibitors of MMP-13 for Arthritic Disorders》, and you may find the article in ACS Omega.Synthetic Route of C5H4IN The information in the text is summarized as follows:
Here, we described the design, by fragment merging and multiparameter optimization, of selective MMP-13 inhibitors that display an appropriate balance of potency and physicochem. properties to qualify as tool compounds suitable for in vivo testing. Optimization of potency was guided by structure-based insights, specifically to replace an ester moiety and introduce polar directional hydrogen bonding interactions in the core of the mol. By introducing polar enthalpic interactions in this series of inhibitors, the overall beneficial physicochem. properties were maintained. These physicochem. properties translated to excellent drug-like properties beyond potency. In a murine model of rheumatoid arthritis, treatment of mice with selective inhibitors of MMP-13 resulted in a statistically significant reduction in the mean arthritic score vs. control when dosed over a 14 day period. The experimental process involved the reaction of 4-Iodopyridine(cas: 15854-87-2Synthetic Route of C5H4IN)
4-Iodopyridine(cas: 15854-87-2) is used as a reagent in the synthesis of indazolylamides as glucocorticoid receptor agonists. 4-Iodopyridine is a halogenated heterocycle that is a building block for proteomics research.Synthetic Route of C5H4IN
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com