1379820-76-4Relevant academic research and scientific papers
Structure-Activity Studies Reveal Scope for Optimisation of Ebselen-Type Inhibition of SARS-CoV-2 Main Protease
Thun-Hohenstein, Siegfried T. D.,Suits, Timothy F.,Malla, Tika R.,Tumber, Anthony,Brewitz, Lennart,Choudhry, Hani,Salah, Eidarus,Schofield, Christopher J.
, (2021/12/30)
The reactive organoselenium compound ebselen is being investigated for treatment of coronavirus disease 2019 (COVID-19) and other diseases. We report structure-activity studies on sulfur analogues of ebselen with the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), employing turnover and protein-observed mass spectrometry-based assays. The results reveal scope for optimisation of ebselen/ebselen derivative- mediated inhibition of Mpro, particularly with respect to improved selectivity.
KOtBu mediated synthesis of phenanthridinones and dibenzoazepinones
Bhakuni, Bhagat Singh,Kumar, Amit,Balkrishna, Shah Jaimin,Sheikh, Javeed Ahmed,Konar, Sanjit,Kumar, Sangit
supporting information; experimental part, p. 2838 - 2841 (2012/07/28)
Synthesis of substituted phenanthridinones and dibenzoazepinones has been realized from 2-halo-benzamides in the presence of potassium tert-butoxide and a catalytic amount of 1,10-phenanthroline or AIBN. This new carbon-carbon bond forming reaction gives direct access to various biaryl lactams containing six- and seven-membered rings chemoselectively. Carbon-carbon coupling seems to proceed by the generation of a radical in the amide ring which leads to C-H arylation of aniline.
