14502-42-2Relevant articles and documents
Azerocyclic compounds and their uses
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Paragraph 0397-0402, (2022/01/20)
The present invention proposes a nitrogen heterocyclic compound and its use, in particular, the present invention proposes a new compound that effectively inhibits ATX, which is a compound shown in the formula below, or a tautomer of the compound shown be
Chiral Mercaptoacetamides Display Enantioselective Inhibition of Histone Deacetylase6 and Exhibit Neuroprotection in Cortical Neuron Models of Oxidative Stress
Kalin, Jay H.,Zhang, Hankun,Gaudrel-Grosay, Sophie,Vistoli, Giulio,Kozikowski, Alan P.
experimental part, p. 425 - 439 (2012/06/04)
Mercaptoacetamide-based ligands have been designed as a new class of histone deacetylase (HDAC) inhibitors for possible use in the treatment of neurodegenerative diseases. The thiol group of these compounds provides a key binding element for interaction with the catalytic zinc ion, and thus differs from the more typically employed hydroxamic acid based zinc binding groups. Herein we disclose the chemistry and biology of some substituted mercaptoacetamides with the intention of increasing HDAC6 isoform selectivity while maintaining potency similar to their hydroxamic acid analogues. The introduction of a stereocenter α to the thiol group was found to have a considerable impact on HDAC inhibitor potency. These new compounds were also profiled for their therapeutic potential in an invitro model of stress-induced neuronal injury and were found to act as nontoxic neuroprotective agents.