117719-16-1Relevant 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)
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.
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia
Bartolomé-Nebreda, José Manuel,Delgado, Francisca,Martín-Martín, María Luz,Martínez-Viturro, Carlos M.,Pastor, Joaquín,Tong, Han Min,Iturrino, Laura,Macdonald, Gregor J.,Sanderson, Wendy,Megens, Anton,Langlois, Xavier,Somers, Marijke,Vanhoof, Greet,Conde-Ceide, Susana
, p. 4196 - 4212 (2014/06/09)
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited select
Discovery and application of iminotriphenylphosphorane as a formal aromatic primary amine protecting group
Delouvrié, Bénédicte,Germain, Hervé,Harris, Craig S.,Lamorlette, Maryannick,Lebraud, Honorine,Nguyen, Ha Thi Hoang,Noisier, Anais,Ouvry, Gilles
supporting information, p. 5380 - 5384 (2012/10/29)
During our efforts to selectively synthesise N-arylated benzotriazole fragments, we developed a new primary aromatic amine protecting group strategy showing significant advantages over recognised protecting groups.