Published in
Royal Society of Chemistry, MedChemComm, 6(8), p. 1246-1254
DOI: 10.1039/c7md00078b
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Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4
Journal article published in 2017 by
José Luis Díaz 
,
Jordi Corbera,
Daniel Martínez ,
Magda Bordas,
Cristina Sicre,
Rosalia Pascual,
Mª José Pretel,
Ana Paz Marín ,
Ana Montero ,
Albert Dordal ,
Inés Alvarez ,
Carmen Almansa
,
Jordi Corbera,
Daniel Martínez ,
Magda Bordas,
Cristina Sicre,
Rosalia Pascual,
Mª José Pretel,
Ana Paz Marín ,
Ana Montero ,
Albert Dordal ,
Inés Alvarez ,
Carmen Almansa
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Abstract
A SAR study identified the 4-(1-methylpyrazol-5-yl) derivative, 12f, as a selective σ1R antagonist with a good ADMET profile and potent antinociception.