22943-93-7Relevant articles and documents
GLYT2 MODULATORS
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Page/Page column 51-52, (2010/02/11)
α-, β-, and γ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I
Novel glycine transporter type-2 reuptake inhibitors. Part 2: β- and γ-amino acid derivatives
Wolin, Ronald L.,Santillán Jr., Alejandro,Barclay, Tristin,Tang, Liu,Venkatesan, Hariharan,Wilson, Sandy,Lee, Doo Hyun,Lovenberg, Timothy W.
, p. 4493 - 4509 (2007/10/03)
Several β- and γ-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [ 14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) were evaluated. A range of lipoph
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors
Wilson, Kenneth J.,Illig, Carl R.,Subasinghe, Nalin,Hoffman, James B.,Jonathan Rudolph,Soll, Richard,Molloy, Christopher J.,Bone, Roger,Green, David,Randall, Troy,Zhang, Marie,Lewandowski, Frank A.,Zhou, Zhao,Sharp, Celia,Maguire, Diane,Grasberger, Bruce,DesJarlais, Renee L.,Spurlino, John
, p. 915 - 918 (2007/10/03)
The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.
