928118-00-7Relevant articles and documents
Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template
Lee, Jeewoo,Tran, Phuong-Thao,Hoang, Van-Hai,Thorat, Shivaji A.,Kim, Sung Eun,Ann, Jihyae,Chang, Yu Jin,Nam, Dong Woo,Song, Hyundong,Mook-Jung, Inhee,Lee, Jiyoun
, p. 3821 - 3830 (2013/07/19)
In an effort to design inhibitors of human glutaminyl cyclase (QC), we have synthesized a library of N-aryl N-(5-methyl-1H-imidazol-1-yl)propyl thioureas and investigated the contribution of the aryl region of these compounds to their structure-activity relationships as cyclase inhibitors. Our design was guided by the proposed binding mode of the preferred substrate for the cyclase. In this series, compound 52 was identified as the most potent QC inhibitor with an IC50 value of 58 nM, which was two-fold more potent than the previously reported lead 2. Compound 52 is a most promising candidate for future evaluation to monitor its ability to reduce the formation of pGlu-Aβ and Aβ plaques in cells and transgenic animals.
Alpha2C adrenoreceptor agonists
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Page/Page column 43, (2010/11/26)
In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.