92001-52-0Relevant articles and documents
Design and optimization of purine derivatives as in vivo active PDE10A inhibitors
Chen, Liu,Chen, Danqi,Tang, Le,Ren, Jing,Chen, Jiaojiao,Zhen, Xuechu,Liu, Yu-Chih,Zhang, Chenhua,Luo, Haibin,Shen, Jingkang,Xiong, Bing
, p. 3315 - 3329 (2017/05/29)
Phosphodiesterases are important enzymes regulating signal transduction mediated by second messenger molecules cAMP or cGMP. PDE10A is a unique member in the PDE family because of its selective expression in medium spiny neurons. It is recognized as anti-psychotic drug target. Based on the structural similarity between our previous chemistry work on 8-aminoimidazo[1,2-a]pyrazines and the PDE10A inhibitors reported by Bartolome-Nebreda et al., we initialized a project for developing PDE10A inhibitors. After several rounds of optimization, we were able to obtain a few compounds with good PDE10A enzymatic activity. And after further PDE enzymatic selectivity study, metabolic stability assay and in vivo pharmacological tests we identified two inhibitors as interesting lead compounds with the potential for further PDE10A lead optimizatioin.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 262, (2012/08/27)
Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Specificity of the 1-Methyladenine Receptors in Starfish Oocytes: Synthesis and Properties of Some 1,8-Disubstituted Adenines, 1,6-Dimethyl-1H-purine, and of the 1-(Azidobenzyl)adenines
Mornet, Rene,Leonard, Nelson J.,Theiler, Jane B.,Doree, Marcel
, p. 879 - 885 (2007/10/02)
A selective synthesis of 1,6-dimethylpurine (16) and the preparations of the 1-(azidobenzyl)adenines (11)-(13), 8-azido-1-benzyladenine (10), and 1-methyladenine derivatives (2)-(9) with various 8-substituents (azido, chloro, bromo, alkyl, and hydroxymeth