Aminoethylenes: A Tetrahedral Intermediate Isostere Yielding Potent Inhibitors of the Aspartyl Protease BACE-1 was written by Yang, Wenjin;Lu, Wanli;Lu, Yafan;Zhong, Min;Sun, Jian;Thomas, Anila E.;Wilkinson, Jennifer M.;Fucini, Raymond V.;Lam, Melissa;Randal, Mike;Shi, Xiao-Ping;Jacobs, Jeffrey W.;McDowell, Robert S.;Gordon, Eric M.;Ballinger, Marcus D.. And the article was included in Journal of Medicinal Chemistry in 2006.Application In Synthesis of Boc-D-Leu-OMe This article mentions the following:
A series of novel β-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing an aminoethylene (AE) tetrahedral intermediate isostere were synthesized and evaluated in comparison to corresponding hydroxyethylene (HE) compounds Enzymic inhibitory values were similar for both isosteres, as were structure-activity relationships with respect to stereochem. preference and substituent variation (P2/P3, P1, and P2′); however, the AE compounds were markedly more potent in a cell-based assay for reduction of β-secretase activity. The incorporation of preferred P2/P3, P1, and P2′ substituents into the AE pharmacophore yielded compound I, which possessed enzymic and cell assay IC50s of 26 nM and 180 nM, resp. A three-dimensional crystal structure of I in complex with BACE-1 revealed that the amino group of the inhibitor core engages the catalytic aspartates in a manner analogous to hydroxyl groups in HE inhibitors. The AE isostere class represents a promising advance in the development of BACE-1 inhibitors. In the experiment, the researchers used many compounds, for example, Boc-D-Leu-OMe (cas: 133467-01-3Application In Synthesis of Boc-D-Leu-OMe).
Boc-D-Leu-OMe (cas: 133467-01-3) belongs to esters. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Liquid esters of low volatility serve as softening agents for resins and plastics. Esters also include many industrially important polymers. Polymethyl methacrylate is a glass substitute sold under the names Lucite and Plexiglas; polyethylene terephthalate is used as a film (Mylar) and as textile fibres sold as Terylene, Fortrel, and Dacron.Application In Synthesis of Boc-D-Leu-OMe
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics