1610340-16-3Relevant academic research and scientific papers
Pyrazolo[3,4-: D] pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4
Díaz, José Luis,Corbera, Jordi,Martínez, Daniel,Bordas, Magda,Sicre, Cristina,Pascual, Rosalia,Pretel, M José,Marín, Ana Paz,Montero, Ana,Dordal, Albert,Alvarez, Inés,Almansa, Carmen
, p. 1246 - 1254 (2017)
The replacement of acylamino by cyclic substituents in the position 4 of the pyrazolo[3,4-d]pyrimidine scaffold, led to highly active sigma-1 receptor (σ1R) ligands. Phenyl or pyrazolyl groups were the best in terms of affinity for the σ1R and the 4-(1-methylpyrazol-5-yl) derivative, 12f, was the most selective. Compound 12f is also one of the best σ1R ligands ever described in terms of lipophilic ligand efficiency, which translates into a good physicochemical and ADMET profile. In addition, 12f was identified as an antagonist of the σ1R in view of its potent antinociceptive profile in several pain models in mice.
