CAS: 58457-32-2; 5-(Oxiran-2-Ylmethoxy)-2,3,4,9-Tetrahydro-1H-Carbazole

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5-羟基-2,3,4,9-四氢咔唑 5-Hydroxy-1,2,3,4-Tetrahydro-Carbazol 35618-96-3

📜5-羟基-2,3,4,9-四氢咔唑,环氧氯丙烷置于sodium Hydroxide体系中,用 二甲基亚砜 作为反应溶剂,化学反应生成 5-(环氧乙烷基甲氧基)-2,3,4,9-四氢咔唑
参考文献:Novel Carvedilol Analogues That Suppress Store-Overload-Induced Ca2+ Release
标题:Novel Carvedilol Analogues That Suppress Store-Overload-Induced Ca2+ Release
摘要:Carvedilol Is A Uniquely Effective Drug For The Treatment Of Cardiac Arrhythmias In Patients With Heart Failure. This Activity Is In Part Because Of Its Ability To Inhibit Store-Overload-Induced Calcium Release (Soicr) Through The Ryr2 Channel. We Describe The Synthesis,Characterization,And Bioassay Of Ca. 100 Compounds Based On The Carvedilol Motif To Identify Features That Correlate With And Optimize Soicr Inhibition. A Single-Cell Bioassay Was Employed On The Basis Of The Ryr2-R4496C Mutant Hek-293 Cell Line In Which Calcium Release From The Endoplasmic Reticulum Through The Defective Channel Was Measured. Ic50 Values For Soicr Inhibition Were Thus Obtained. The Compounds Investigated Contained Modifications To The Three Principal Subunits Of Carvedilol,Including The Carbazole And Catechol Moieties,As Well As The Linker Chain Containing The Beta-Amino Alcohol Functionality. The Sar Results Indicate That Significant Alterations Are Tolerated In Each Of The Three Subunits.
DOI:10.1021/jm401090A