81279-39-2Relevant articles and documents
Practical silyl protection of ribonucleosides
Blaisdell, Thomas P.,Lee, Sunggi,Kasaplar, Pinar,Sun, Xixi,Tan, Kian L.
supporting information, p. 4710 - 4713 (2013/10/08)
Herein we report the site-selective silylation of the ribonucelosides. The method enables a simple and efficient procedure for accessing suitably protected monomers for automated RNA synthesis. Switching to the opposite enantiomer of the catalyst allows f
ppGpp analogues inhibit synthetase activity of Rel proteins from Gram-negative and Gram-positive bacteria
Wexselblatt, Ezequiel,Katzhendler, Jehoshua,Saleem-Batcha, Raspudin,Hansen, Guido,Hilgenfeld, Rolf,Glaser, Gad,Vidavski, Roee R.
scheme or table, p. 4485 - 4497 (2010/08/22)
A prominent feature of the stringent response is the accumulation of two unusual phosphorylated derivatives of GTP and GDP (pppGpp: 5′-triphosphate-3′-diphosphate, and ppGpp: 5′-3′-bis-diphosphate), collectively called (p)ppGpp, within a few seconds after the onset of amino-acid starvation. The synthesis of these 'alarmone' compounds is catalyzed by RelA homologues. Other features of the stringent response include inhibition of stable RNA synthesis and modulation of transcription, replication, and translation. (p)ppGpp accumulation is important for virulence induction, differentiation and antibiotic resistance. We have synthesized a group of (p)ppGpp analogues and tested them as competitive inhibitors of Rel proteins in vitro. 2′-Deoxyguanosine-3′-5′-di(methylene bisphosphonate) [compound (10)] was found as an inhibitor that reduces ppGpp formation in both Gram-negative and Gram-positive bacteria. In silico docking together with competitive inhibition analysis suggests that compound (10) inhibits activity of Rel proteins by competing with GTP/GDP for its binding site. As Rel proteins are completely absent in mammalians, this appears to be a very attractive approach for the development of novel antibacterial agents.
An efficient preparation of protected ribonucleosides for phosphoramidite RNA synthesis
Serebryany, Vladimir,Beigelman, Leonid
, p. 1983 - 1985 (2007/10/03)
An efficient synthesis of protected ribonucleosides useful for phosphoramidite RNA synthesis is described. Di-t-butylsilylene group was employed for simultaneous protection of 3′- and 5′-hydroxyl functions of nucleoside. Subsequent silylation of free 2′-O
