Zhao, Siqi; Zhang, Han; Jin, Hongwei; Cai, Xiaobo; Zhang, Rongxue; Jin, Zefang; Yang, Wei; Yu, Peilin; Zhang, Liangren; Liu, Zhenming published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specific inhibitors》.Quality Control of Benzyl 2-bromoacetate The article contains the following contents:
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. In addition to this study using Benzyl 2-bromoacetate, there are many other studies that have used Benzyl 2-bromoacetate(cas: 5437-45-6Quality Control of Benzyl 2-bromoacetate) was used in this study.
Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is a synthetic chemical produced for industry from benzyl alcohol and acetic acid, but is also naturally present in the essential oils of many plants, including jasmine and ylang ylang.Quality Control of Benzyl 2-bromoacetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary