3346-63-2Relevant articles and documents
Novel nucleoside analogues targeting HCV replication through an NS5A-dependent inhibition mechanism
Lougiakis, Nikolaos,Frakolaki, Efseveia,Karmou, Panagiota,Pouli, Nicole,Marakos, Panagiotis,Madan, Vanesa,Bartenschlager, Ralf,Vassilaki, Niki
, p. 352 - 367 (2017)
A series of new tricyclic nucleosides were synthesized and evaluated as hepatitis C virus (HCV) replication inhibitors. Initial screening in a HCV replicon system, derived from a genotype 1b isolate, identified 9-benzylamino-3-(β-D-ribofuranosyl)-3H-imidazo[4′,5′:5,6]pyrido[2,3-b]pyrazine (15d) as the most potent analogue. Comparative assessment of 15d activity against HCV full-length viruses or subgenomic replicons derived from genotypes 1 to 4 revealed a specificity of the compound for genotypes 1 and 3. Surprisingly, resistance mutations selected against 15d were mapped to domains II and III of the non-structural protein 5A (NS5A), but not to the RNA-dependent RNA polymerase residing in NS5B. These results argue that compound 15d might represent a lead for the development of a novel class of NS5A inhibitors.
p38α AUTOPHOSPHORYLATION INHIBITORS
-
Page/Page column 34, (2020/07/07)
The present invention concerns inhibitors of p38α autophosphorylation, pharmaceutical compositions comprising them, and their use in the treatment of a number of diseases, such as myocardial ischemia reperfusion injury. The inhibitors satisfy the following general formula: wherein R, R1, R2, R4, and R5 may have different meanings.
A practical synthesis of substituted 2,6-diaminopyridines via microwave-assisted copper-catalyzed amination of halopyridines
Mastalir, Matthias,Rosenberg, Egon E.,Kirchner, Karl
, p. 8104 - 8110 (2015/12/30)
A microwave assisted copper-catalyzed amination protocol is reported utilizing a series of 2,6-dihalo- and 2-amino-6-halo pyridine precursors. Using this procedure, selective substitution of one or two halogens by aryl or alkylamines was achieved within 2-6 h with temperatures between 80 and 225 °C affording 2,6-diaminopyridines in good to excellent isolated yields. The reaction allows easy variation between educts and different N-substitutions. The target compounds are valuable precursors for the synthesis of bis-phosphorylated 2,6-diaminopyridines which are used as PNP pincer ligands in transition metal complexes.