96237-92-2Relevant academic research and scientific papers
Structure-Activity Studies Reveal Scope for Optimisation of Ebselen-Type Inhibition of SARS-CoV-2 Main Protease
Brewitz, Lennart,Choudhry, Hani,Malla, Tika R.,Salah, Eidarus,Schofield, Christopher J.,Suits, Timothy F.,Thun-Hohenstein, Siegfried T. D.,Tumber, Anthony
supporting information, (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.
Substitution Reactions of Phenylated Aza-Heterocycles. Part 2. Bromination of Some 2,5-Diaryl-1,3,4-oxadiazoles
Blackhall, Alexander,Brydon, Donald L.,Javaid, Khalid,Sagar, Anthony J. G.,Smith, David M.
, p. 3485 - 3497 (2007/10/02)
Electrophilic bromination of the title compounds may be achieved using either bromine in oleum, or bromine and potassium bromate in a sulphuric-acetic acid mixture.Under the milder reaction conditions provided by the latter, 2-(p-nitrophenyl)-5-phenyl-1,3,4-oxadiazole (2), the model compound used in this study, is mono- and di-brominated in the phenyl ring.In the first bromination step, all three monobromo-isomers are produced in appreciable amount.The orientation of the second bromination is controlled entirely by the first bromine and not by the oxadiazole substituent: this is confirmed by a separate study of the bromination of the three monobromo-compounds (3a-3c).
