99857-43-9Relevant academic research and scientific papers
Substrate and Catalyst Effects in the Enantioselective Copper-Catalysed C–H Insertion Reactions of α-Diazo-β-oxo Sulfones
Shiely, Amy E.,Clarke, Leslie-Ann,Flynn, Christopher J.,Buckley, Aoife M.,Ford, Alan,Lawrence, Simon E.,Maguire, Anita R.
supporting information, p. 2277 - 2289 (2018/06/04)
Excellent enantioselectivities of up to 98 % ee are achieved by employing the copper-bis(oxazoline)-NaBARF catalyst system in the C–H insertion reactions of α-diazo-β-oxo sulfones. The influence of variation of the bis(oxazoline) ligand, copper salt, additive and substrate on both the efficiency and the enantioselectivities of these intramolecular C–H insertion reactions has been explored. Optimum enantioselectivities are achieved with phenyl and diphenyl ligands across the substrate series.
Structural determinants for histamine H1 affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs
Aslanian, Robert,Piwinski, John J.,Zhu, Xiaohong,Priestley, Tony,Sorota, Steve,Du, Xiao-Yi,Zhang, Xue-Song,McLeod, Robbie L.,West, Robert E.,Williams, Shirley M.,Hey, John A.
supporting information; experimental part, p. 5043 - 5047 (2010/03/31)
In the late 1980's reports linking the non-sedating antihistamines terfenadine and astemizole with torsades de pointes, a form of ventricular tachyarrhythmia that can degenerate into ventricular fibrillation and sudden death, appeared in the clinical literature. A substantial body of evidence demonstrates that the arrhythmogenic effect of these cardiotoxic antihistamines, as well as a number of structurally related compounds, results from prolongation of the QT interval due to suppression of specific delayed rectifier ventricular K+ currents via blockade of the hERG-IKr channel. In order to better understand the structural requirements for hERG and H1 binding for terfenadine, a series of analogs of terfenadine has been prepared and studied in both in vitro and in vivo hERG and H1 assays.
