《Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation》 was published in Bioorganic & Medicinal Chemistry Letters in 2020. These research results belong to Shang, Yanguo; Hao, Qingjing; Jiang, Kaixuan; He, Mengting; Wang, Jinxin. Safety of Methyl 2-chloro-2-oxoacetate The article mentions the following:
Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat pain, inflammation, and other central nervous system disorders. Herein, a series of novel heterocyclic carbohydrazide derivatives were firstly designed by the classic scaffold-hopping strategy. Then, multi-steps synthesis and human FAAH enzyme inhibiting activity assays were conducted. Among them, compound I showed strong inhibition against human FAAH with IC50 of 2.8μM. Corresponding docking studies revealed that the acyl hydrazide group of compound I well-occupied the acyl-chain binding pocket. It also exhibited high selectivity towards FAAH when comparing with CES2 and MAGL. Addnl., compound I effectively suppressed the LPS-induced neuroinflammation of microglial cells (BV2) via the reduction of interleukin-1β and tumor necrosis factor-α. Our results provided significative lead compounds for the further discovery of novel selective and safe FAAH inhibitors with potent anti-neuroinflammation activity.Methyl 2-chloro-2-oxoacetate(cas: 5781-53-3Safety of Methyl 2-chloro-2-oxoacetate) was used in this study.
Methyl 2-chloro-2-oxoacetate(cas: 5781-53-3) belongs to acyl chlorides. In the laboratory, acyl chlorides are generally prepared by treating carboxylic acids with thionyl chloride (SOCl2). The reaction is catalyzed by dimethylformamide and other additives.Safety of Methyl 2-chloro-2-oxoacetate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics