In 2017,Lv, Wei; Zhang, Guangming; Barinka, Cyril; Eubanks, James H.; Kozikowski, Alan P. published 《Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors》.ACS Medicinal Chemistry Letters published the findings.Related Products of 51644-96-3 The information in the text is summarized as follows:
A series of non-hydroxamate HDAC6 inhibitors were prepared in our effort to develop potent and selective compounds for possible use in Central Nervous System (CNS) disorders, thus obviating the genotoxicity often associated with the hydroxamates. Halogens are incorporated in the cap groups of the designed mercaptoacetamides in order to increase brain accessibility. The indole analog and quinoline analog displayed potent HDAC6 inhibitory activity (IC50 11 nM and 2.8 nM) and excellent selectivity against HDAC1. Both compounds, together with their ester prodrug and disulfide prodrugs were found to be effective in promoting tubulin acetylation in HEK cells. The disulfide prodrugs also released a stable concentration of the indole and quinoline analogs upon microsomal incubation. Administration of disulfide prodrugs in vivo was found to trigger an increase of tubulin acetylation in mouse cortex. These results suggest that further exploration of these com-pounds for the treatment of CNS disorders is warranted. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)
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).Related Products of 51644-96-3
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