In 2022,Liu, Guodong; Hou, Ruilin; Xu, Lijuan; Zhang, Xinqi; Yan, Jianyu; Xing, Chengguo; Xu, Ke; Zhuang, Chunlin published an article in Journal of Medicinal Chemistry. The title of the article was 《Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides》.Safety of 2-Bromoacetamide The author mentioned the following in the article:
Directly inhibiting the Keap1-Nrf2 protein-protein interaction has been investigated as a promising strategy to activate Nrf2 for anti-inflammation. We previously reported a naphthalensulfonamide Keap1-Nrf2 inhibitor NXPZ-2, but have not determined the exact binding mode with Keap1. This sym. naphthalenesulfonamide compound has relatively low solubility Herein, we first determined a crystal complex (resolution: 2.3 Å) of human Keap1 Kelch domain with NXPZ-2. Further optimizations on the solvent exposed region obtained asym. naphthalenesulfonamides and three crystal structures of Keap1 in complex with designed compounds Among them, the asym. piperazinyl-naphthalenesulfonamide 6k with better aqueous solubility showed the best KD2 value of 0.21μM to block the interaction. The productions of ROS and NO and the expression of TNF-α were inhibited by 6k in the in vitro model. This compound could relieve inflammations by significantly increasing the Nrf2 nuclear translocation in the LPS-induced ALI model with promising pharmacokinetic properties. In the experiment, the researchers used many compounds, for example, 2-Bromoacetamide(cas: 683-57-8Safety of 2-Bromoacetamide)
2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Safety of 2-Bromoacetamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics