New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy
一种新型咪唑并二氮杂卓类似物,5-(8-溴-6-(吡啶-2-基)-4H-苯并[f]咪唑并[1,5-a][1,4]二氮杂卓-3-基)噁唑,具有合成路线简化、口服血浆和脑暴露量高等优点,在小鼠中表现出抗癫痫疗效,并在内侧颞叶癫痫患者脑片的神经网络中表现出抗癫痫发生活性。
期刊:ACS Chemical Neuroscience
影响因子:3.9
doi:10.1021/acschemneuro.3c00555
Sharmin, Dishary; Divović, Branka; Ping, Xingjie; Cerne, Rok; Smith, Jodi L; Rezvanian, Sepideh; Mondal, Prithu; Meyer, Michelle Jean; Kiley, Molly E; Arnold, Leggy A; Mian, Md Yeunus; Pandey, Kamal P; Jin, Xiaoming; Mitrović, Jelena R; Djorović, Djordje; Lippa, Arnold; Cook, James M; Golani, Lalit K; Scholze, Petra; Savić, Miroslav M; Witkin, Jeffrey M