High-throughput screening for a SARS-CoV-2 frameshifting inhibitor using a cell-free protein synthesis system.

Programmed-1 ribosomal frameshifting (-1 PRF) is a translational mechanism adopted by some viruses, including SARS-CoV-2. To find a compound that can inhibit -1 PRF in SARS-CoV-2, we set up a high-throughput screening system using a HeLa cell extract-derived cell-free protein synthesis (CFPS) system. A total of 32,000 compounds were individually incubated with the CFPS system programmed with a -1 PRF-EGFP template. Several compounds were observed to decrease the -1 PRF-driven fluorescence, and one of them had some suppressive effect on -1 PRF of a SARS-CoV-2 genome sequence in transfected cells. Thus the CFPS system can be used as a tool for a high-throughput screening of chemicals.

Highly regio- and stereocontrolled preparation of α-(trifluoromethyl)-ß-(phenylthio) enamines by the hydroamination of in situ-synthesized 1-(trifluoromethyl)-2-(phenylthio)ethyne.

Various nitrogen nucleophiles were easily added to in situ-generated 1-(trifluoromethyl)-2-(phenylthio)ethyne to afford the corresponding trifluoromethyl enamines in good-to-high yields and with high regio- and stereocontrol under very mild conditions.

Regio- and stereoselective synthesis of tetrasubstituted (E)-(2-chloro-2-fluoro-1-iodovinyl)dimethylphenylsilane and its desilylative sonogashira coupling.

Trihalo-substituted vinylsilane was readily synthesized in 77% yield and in an excellent regio- and stereoselective manner from in situ-generated fluorosilylacetylene, followed by the addition of I2 and NCS. The silane was committed to sequential Sonogashira coupling with various terminal acetylenes under mild conditions, affording desilylated chlorofluoro-enyne adducts in moderate to good yields.

Application of thermography in dentistry--visualization of temperature distribution on oral tissues.

The purpose of this study was to devise and propose appropriate conditions for the photographing of thermal images in the oral cavity and to evaluate which thermography techniques can be applied to dentistry by evaluating the differences in temperature among oral tissues. Thermal images of oral cavities of 20 volunteers in normal oral condition were taken according to the guidelines of the Japanese Society of Thermography, with five added items for oral observation. The use of a mirror made it possible to take thermal images of the posterior portion or palate. Teeth, free gingiva, attached gingiva and alveolar mucosa were identified on thermal images. There were differences in temperature between teeth, free gingiva, attached gingiva and alveolar mucosa. These were nearly in agreement with the anatomical view. Thermography need no longer be restricted to the anterior portion using a mirror, and can now be applied to the dental region.