In 2017,Ding, Xiao; Dai, Xuedong; Long, Kai; Peng, Cheng; Andreotti, Daniele; Bamborough, Paul; Eatherton, Andrew J.; Edge, Colin; Jandu, Karamjit S.; Nichols, Paula L.; Philps, Oliver J.; Stasi, Luigi Piero; Wan, Zehong; Xiang, Jia-Ning; Dong, Kelly; Dossang, Pamela; Ho, Ming-Hsun; Li, Yi; Mensah, Lucy; Guan, Xiaoming; Reith, Alastair D.; Ren, Feng published 《Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Electric Literature of C10H17BN2O2 The information in the text is summarized as follows:
Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson’s disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds I, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Electric Literature of C10H17BN2O2)
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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Electric Literature of C10H17BN2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics