Burmistrov Vladimir V, Morisseau Christophe, Shkineva Tatyana K, Danilov Dmitry V, Gladkikh Boris, Butov Gennady M, Fayzullin Robert R, Dutova Tatyana Ya, Hammock Bruce D, Dalinger Igor L
Department of Entomology and Nematology, and Comprehensive Cancer Center, University of California, Davis, CA, 95616, USA.
Department of Chemistry, Technology and Equipment of Chemical Industry, Volzhsky Polytechnic Institute (branch) Volgograd State Technical University, 42a Engels Street, Volzhsky, 404121, Russia.
J Fluor Chem. 2023 Feb;266. doi: 10.1016/j.jfluchem.2023.110087. Epub 2023 Jan 16.
A series of soluble epoxide hydrolase (sEH) inhibitors containing halogenated pyrazoles was developed. Inhibition potency of the obtained compounds ranges from 0.8 to 27.5 nM. 1-Adamantyl-3-[(4,5-dichloro-1-methyl-1Н-pyrazol-3-yl)methyl]urea (, IC = 0.8 nM) and 1-[(Adamantan-1-yl)methyl]-3-[(4,5-dichloro-1-methyl-1Н-pyrazol-3-yl)methyl]urea (, IC = 1.2 nM) were found to be the most potent sEH inhibitors within the described series.
开发了一系列含卤代吡唑的可溶性环氧化物水解酶（sEH）抑制剂。所得化合物的抑制活性范围为0.8至27.5 nM。发现1-金刚烷基-3-[(4,5-二氯-1-甲基-1H-吡唑-3-基)甲基]脲（，IC = 0.8 nM）和1-[(金刚烷-1-基)甲基]-3-[(4,5-二氯-1-甲基-1H-吡唑-3-基)甲基]脲（，IC = 1.2 nM）是所述系列中最有效的sEH抑制剂。
