Zhang, Han; Liu, Huan; Luo, Xiao; Wang, Yuxi; Liu, Yuan; Jin, Hongwei; Liu, Zhenming; Yang, Wei; Yu, Peilin; Zhang, Liangren; Zhang, Lihe published the artcile< Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors>, COA of Formula: C7H7BrN2O, the main research area is dihydroquinazolinone preparation SAR human TRPM2 inhibitor; 2,3-Dihydroquinazolin-4(1H)-ones; Inhibitors; SAR; TRPM2; Virtual screening.
In this study, a series of novel 2,3-dihydroquinazolin-4(1H)-one derivatives, e.g. I was subsequently synthesized and characterized. Their inhibitory activity against the TRPM2 channel was evaluated by calcium imaging and electrophysiol. approaches. Some of the compounds exhibited significant inhibitory activity, especially 6-bromo-8-methyl-2-[3-(2-naphthyl)-1H-pyrazol-4-yl]-2,3-dihydro-1H-quinazolin-4-one which showed an IC50 of 3.7μM against TRPM2 and did not affect the TRPM8 channel. The summarized structure-activity relationship (SAR) provided valuable insights for further development of specific TRPM2 targeted inhibitors.
European Journal of Medicinal Chemistry published new progress about Homo sapiens. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, COA of Formula: C7H7BrN2O.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics