497848-13-2Relevant academic research and scientific papers
Discovery of BI 99179, a potent and selective inhibitor of type i fatty acid synthase with central exposure
Kley, J?rg T.,MacK, Jürgen,Hamilton, Bradford,Scheuerer, Stefan,Redemann, Norbert
scheme or table, p. 5924 - 5927 (2011/10/09)
Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats.
BETA-AMYLOID PET IMAGING AGENTS
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Page/Page column 38; 40, (2008/06/13)
Novel derivatives of imidazopyridinylbenzeneamines and novel derivatives of benzothiazolylbenzeneamines are disclosed that offer improved behavior when used as imaging agents for positron emission tomography of beta-amyloids. Also disclosed is a palladium-catalyzed reaction scheme under microwave conditions for aryl thioethers in general that provides a high ratio of substitution relative to reduction and can be used for the imidazopyridinylbenzeneamine derivatives as well as other compounds of related structure.
Rapid palladium-catalyzed cross-coupling in the synthesis of aryl thioethers under microwave conditions
Cai, Lisheng,Cuevas, Jessica,Peng, Yi-Yuan,Pike, Victor W.
, p. 4449 - 4452 (2007/10/03)
A Pd-catalyzed coupling of aromatic iodides or bromides and tin-thiolates under microwave conditions was developed to synthesize aromatic thioethers without concomitant formation of the reduced products. Ligand screening revealed DiPPF and BINAP-Tol as th
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting β-amyloid plaques in the brain
Zhuang, Zhi-Ping,Kung, Mei-Ping,Wilson, Alan,Lee, Chi-Wan,Pl?ssl, Karl,Hou, Catherine,Holtzman, David M.,Kung, Hank F.
, p. 237 - 243 (2007/10/03)
A series of novel β-amyloid (Aβ) aggregate-specific ligands, 2-(4′-dimethylaminophenyl)-6-iodoimidazo[1,2-a]pyridine, 16(IMPY), and its related derivatives were prepared. An in vitro binding study with preformed Aβ aggregates showed that 16(IMPY) and its
