Zhang, Jianmin; Huitema, Carly; Niu, Chunying; Yin, Jiang; James, Michael N. G.; Eltis, Lindsay D.; Vederas, John C. published the artcile< Aryl methylene ketones and fluorinated methylene ketones as reversible inhibitors for severe acute respiratory syndrome (SARS) 3C-like proteinase>, Related Products of 22620-34-4, the main research area is aryl methylene ketone derivative preparation SARS 3C proteinase inhibitor; fluorinated methylene ketone derivative preparation SARS 3C proteinase inhibitor; structure activity SARS 3C like proteinase inhibiting ketone derivative.
The severe acute respiratory syndrome (SARS) virus depends on a chymotrypsin-like cysteine proteinase (3CLpro) to process the translated polyproteins to functional viral proteins. This enzyme is a target for the design of potential anti-SARS drugs. A series of ketones and corresponding mono- and di-fluoro ketones having two or three aromatic rings were synthesized as possible reversible inhibitors of SARS 3CLpro. The design was based on previously established potent inhibition of the enzyme by oxa analogs (esters), which also act as substrates. Structure-activity relationships and modeling studies indicate that three aromatic rings, including a 5-bromopyridin-3-yl moiety, are key features for good inhibition of SARS 3CLpro. 2-(5-Bromopyridin-3-yl)-1-(5-(4-chlorophenyl)furan-2-yl)ethanone and its α-monofluorinated analog, gave the best reversible inhibition with IC50 values of 13 μM and 28 μM, resp. In contrast to inhibitors having two aromatic rings, α-fluorination of compounds with three rings unexpectedly decreased the inhibitory activity.
Bioorganic Chemistry published new progress about Antiviral agents. 22620-34-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H6ClNO, Related Products of 22620-34-4.
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Alcohols – Chemistry LibreTexts