《Identification of Highly Selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors by a Covalent Fragment-Based Approach》 was written by Huang, Fubao; Hu, Hangchen; Wang, Kai; Peng, Chengyuan; Xu, Wenwei; Zhang, Yu; Gao, Jing; Liu, Yishen; Zhou, Hu; Huang, Ruimin; Li, Minjun; Shen, Jianhua; Xu, Yechun. Quality Control of tert-Butyl (5-aminopentyl)carbamate And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
Covalent ligands are of great interest as therapeutic drugs or biochem. tools. Here, we reported the discovery of highly selective and irreversible inhibitors of lipoprotein-associated phospholipase A2 (Lp-PLA2) using a covalent fragment-based approach. The crystal structure of Lp-PLA2 in complex with a covalent fragment not only reveals the covalent reaction mechanism but also provides a good starting point to design compound 8, which has a more than 130,000-fold and 3900-fold increase in potency and selectivity, resp., compared to those of the covalent fragment. Furthermore, fluorescent probes with high selectivity and sensitivity are developed to characterize Lp-PLA2 and its enzymic activity in vitro or even in living cells in a way more convenient than immunoblotting tests or immunofluorescence imaging. Overall, we provide a paradigm for application of the covalent fragment-based strategy in covalent ligand discovery and the advantage of enol-cyclocarbamate as a new warhead in designing covalent inhibitors of serine hydrolases. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Quality Control of tert-Butyl (5-aminopentyl)carbamate)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Quality Control of tert-Butyl (5-aminopentyl)carbamate
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