Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 70-23-5, is researched, Molecular C5H7BrO3, about Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specific inhibitors, the main research direction is benzoimidazoimidazole preparation TRPM2 channel inhibitor; 2-APB; Inhibitors; SAR; Transient receptor potential melastatin 2 (TRPM2) channel; benzo[d]imidazo[1,2-a]imidazole.Quality Control of Ethyl 3-bromo-2-oxopropanoate.
Transient receptor potential melastatin 2 (TRPM2) channel is associated with ischemia/reperfusion injury, inflammation, cancer and neurodegenerative diseases. However, the lack of specific inhibitors impedes the development of TRPM2 targeted therapeutic agents. To develop a selective TRPM2 inhibitor, three-dimensional similarity-based screening strategy was employed using the energy-minimized conformation of non-selective TRPM2 inhibitor 2-APB as the query structure, which resulted in the discovery of a novel tricyclic TRPM2 inhibitor I with benzo[d]imidazo[1,2-a]imidazole skeleton. A series of I derivatives were subsequently synthesized and evaluated using calcium imaging and electrophysiol. approaches. Among them, preferred compounds II and III inhibited the TRPM2 channel with micromolar half-maximal inhibitory concentration values and exhibited TRPM2 selectivity over the TRPM8 channel, TRPV1 channel, InsP3 receptor and Orai channel. The anal. of structure-activity relationship provides valuable insights for further development of selective TRPM2 inhibitors. Neuroprotection assay showed that II and III could effectively reduce the mortality of SH-SY5Y cells induced by H2O2. These findings enrich the structure types of existing TRPM2 inhibitors and might provide a new tool for the study of TRPM2 function in Reactive oxygen species (ROS) -related diseases.
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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem