Category: triazolesIn 2016 ,《Design, synthesis and biological evaluation of pyrido[2,3-d]pyrimidin-7-(8H)-ones as HCV inhibitors》 appeared in European Journal of Medicinal Chemistry. The author of the article were Camarasa, Marta; Puig de la Bellacasa, Raimon; Gonzalez, Alex L.; Ondono, Raul; Estrada, Roger; Franco, Sandra; Badia, Roger; Este, Jose; Martinez, Miguel Angel; Teixido, Jordi; Clotet, Bonaventura; Borrell, Jose I.. The article conveys some information:
The design and selection of a combinatorial library of pyrido[2,3-d]pyrimidin-7(8H)-ones allowed the synthesis of 121 compounds, using known and new synthetic methodologies and the evaluation of the inhibitory activity against hepatitis C virus (HCV) genotype 1b replicon. Among these compounds, I and II presented very high activities [EC50 = 0.027 μM (CC50 = 5.3 μM) and EC50 = 0.034 μM (CC50 = 13.5 μM), resp.] and high selectivity indexes, 196 and 397. These values are similar to the EC50 reported for sofosbuvir (2) (0.048 μM) using a similar methodol. approach and the same virus subtype. Compounds I and II and were obtained through shorter synthetic itineraries than sofosbuvir and II was achiral contrary to sofosbuvir which presented 4 stereogenic centers. In-silico studies suggested that I and II inhibited NS5B polymerase through allosteric site binding. In the experiment, the researchers used ((1H-Benzo[d][1,2,3]triazol-1-yl)oxy)tris(dimethylamino)phosphonium hexafluorophosphate(V)(cas: 56602-33-6Category: triazoles)
((1H-Benzo[d][1,2,3]triazol-1-yl)oxy)tris(dimethylamino)phosphonium hexafluorophosphate(V)(cas: 56602-33-6) is used as a reagent for peptide coupling, lactonization, selective esterification, amidation of alfa amino acids without racemization and synthesis of magnolamide for antioxidative activity and catalyst for 9-acridinecaroboxamide derivative. It is also used as a precursor for the synthesis of phenyl esters of amino acids.Category: triazoles
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics