In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published 《Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4》.MedChemComm published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:
The replacement of acylamino group by cyclic substituents in the position 4 of the pyrazolo[3,4-d]pyrimidine scaffold I [R = Ph, pyridin-3-yl, 1-methyl-1H-pyrazol-5-yl, etc.], led to highly active sigma-1 receptor (σ1R) ligands. Ph or pyrazolyl groups were the best in terms of affinity for the σ1R and the compound I [R = 1-methyl-1H-pyrazol-5-yl], was the most selective. Compound I [R = 1-methyl-1H-pyrazol-5-yl] was also one of the best σ1R ligands ever described in terms of lipophilic ligand efficiency, which translated into a good physicochem. and ADMET profile. In addition, compound I [R = 1-methyl-1H-pyrazol-5-yl] was identified as an antagonist of the σ1R in view of its potent antinociceptive profile in several pain models in mice.1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole) was used in this study.
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics