16268-88-5Relevant academic research and scientific papers
Strategies for protecting and manipulating triazine derivatives
Hollink, Emily,Simanek, Eric E.,Bergbreiter, David E.
, p. 2005 - 2008 (2007/10/03)
Aminotriazine derivatives are available in two steps by treating chlorotriazines with acid-labile benzylic amines including triphenylmethylamine, diphenylmethylamine, and 2,4-dimethoxybenzyl-amine (Dmb-amine), followed by deprotection using trifluoroaceti
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis
Hajduk, Philip J.,Dinges, Jürgen,Schkeryantz, Jeffrey M.,Janowick, David,Kaminski, Michele,Tufano, Michael,Augeri, David J.,Petros, Andrew,Nienaber, Vicki,Zhong, Ping,Hammond, Rachel,Coen, Michael,Beutel, Bruce,Katz, Leonard,Fesik, Stephen W.
, p. 3852 - 3859 (2007/10/03)
The Erm family of methyltransferases confers resistance to the macrolide-lincosamide-streptogramin type B (MLS) antibiotics through the methylation of 23S ribosomal RNA. Upon the methylation of RNA, the MLS antibiotics lose their ability to bind to the ribosome and exhibit their antibiotic activity. Using an NMR-based screen, we identified a series of triazinecontaining compounds that bind weakly to ErmAM. These initial lead compounds were optimized by the parallel synthesis of a large number of analogues, resulting in compounds which inhibit the Erm-mediated methylation of rRNA in the low micromolar range. NMR and X-ray structures of enzyme/inhibitor complexes reveal that the inhibitors bind to the S- adenosylmethionine binding site on the Erm protein. These compounds represent novel methyltransferase inhibitors that serve as new leads for the reversal of Erm-mediated MLS antibiotic resistance.
Reaction of disubstituted cyanamides with formamides under high pressure
Shibuya, Isao,Oishi, Akihiro,Yasumoto, Masahiko
, p. 1659 - 1662 (2007/10/03)
High pressure-assisted co-cyclization of disubstituted cyanamides with formamide or monosubstituted formamides gave 2-amino- or 2-monosubstituted amino-4,6-bis(disubstituted amino)-1,3,5-triazines in one pot.
