Chen, Liu published the artcileDesign and optimization of purine derivatives as in vivo active PDE10A inhibitors, Application In Synthesis of 51656-68-9, the publication is Bioorganic & Medicinal Chemistry (2017), 25(13), 3315-3329, database is CAplus and MEDLINE.
Phosphodiesterases are important enzymes regulating signal transduction mediated by second messenger mols. 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 chem. 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 enzymic activity. And after further PDE enzymic selectivity study, metabolic stability assay and in vivo pharmacol. tests we identified two inhibitors as interesting lead compounds with the potential for further PDE10A lead optimization.
Bioorganic & Medicinal Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Application In Synthesis of 51656-68-9.
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