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The synthesis of a new series of 4-acylaminopyrazolo[3,4- d ]pyrimidines active on the sigma-1 receptor (σ 1 R) is reported. Compounds were efficiently prepared using a two to three step process starting from commercially available 1 H -pyrazolo[3,4- d ]pyrimidin-4-amine. A SAR study shows that the σ 1 R requires the presence of relatively highly lipophilic substituents at opposite sides of the central scaffold, while selectivity versus the σ 2 R can be improved by shortening the distance of the basic nitrogen to it. Compound 9a was among the most active and selective in vitro derivatives and exhibited potent antinociceptive properties in several pain models in mice, indicating its antagonistic behaviour.

Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 1: 4-acylamino derivatives