27383-86-4Relevant articles and documents
Visible-Light-Induced Aerobic Oxidative Csp3?H Functionalization of Glycine Derivatives for 2-Substituted Benzoxazoles
Zhu, Zhi-Qiang,Liu, Shan,Hu, Zhi-Yu,Xie, Zong-Bo,Tang, Juan,Le, Zhang-Gao
, p. 2568 - 2572 (2021)
We report a simple oxidative Csp3?H functionalization reaction of glycine derivatives by visible-light photoredox catalysis. A wide range of glycine derivatives readily undergo the oxidative cyclization to afford various 2-substituted benzoxazoles. Importantly, this photocatalytic intramolecular dehydrogenative coupling reaction allows for the C?H functionalization of glycine derivatives involving short peptides under mild conditions, which may have value in preparing peptide-derived pharmacologically active molecules. (Figure presented.).
2-substituted benzoxazole compound
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Paragraph 0012; 0020-0023, (2021/03/13)
The invention discloses a 2-substituted benzoxazole compound which is characterized in that the structural formula of the 2-substituted benzoxazole compound is shown as a formula (I), in the formula,R1 is a hydrogen atom, an electron donating group or an electron withdrawing group, R1 is connected with phenyl, and R2 is an alkoxy group or a substituted amino group. The synthesis method comprisesthe following steps: in the presence of a photosensitizer and a transition metal salt, irradiating an N-arylglycine derivative (I) at room temperature through visible light in an organic solvent, performing stirring and reacting for 12-16 hours until TLC (Thin Layer Chromatography) detection reaction is complete, concentrating the reaction solution, and carrying out column chromatography separation to obtain the product 2-substituted benzoxazole (II).
Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation
Hao, Qingjing,He, Mengting,Jiang, Kaixuan,Shang, Yanguo,Wang, Jinxin
supporting information, (2020/04/08)
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 26 showed strong inhibition against human FAAH with IC50 of 2.8 μM. Corresponding docking studies revealed that the acyl hydrazide group of compound 26 well-occupied the acyl-chain binding pocket. It also exhibited high selectivity towards FAAH when comparing with CES2 and MAGL. Additionally, compound 26 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.
