《Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase》 was written by Massari, Serena; Bertagnin, Chiara; Pismataro, Maria Chiara; Donnadio, Anna; Nannetti, Giulio; Felicetti, Tommaso; Di Bona, Stefano; Nizi, Maria Giulia; Tensi, Leonardo; Manfroni, Giuseppe; Loza, Maria Isabel; Sabatini, Stefano; Cecchetti, Violetta; Brea, Jose; Goracci, Laura; Loregian, Arianna; Tabarrini, Oriana. Application of 683-57-8This research focused ontriazolopyrimidine carboxamide preparation antiviral SAR viral protein PB1; Influenza virus; PA-PB1 heterodimerization; Protein-protein interaction; RNA-Dependent RNA polymerase. The article conveys some information:
In search for new anti-Influenza viruses (Flu) drugs, authors have focused on viral RNA-dependent RNA polymerase (RdRP) developing disruptors of PA-PB1 subunits interface with the best compounds characterized by cycloheptathiophene-3-carboxamide and 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide scaffolds. By merging these moieties, two very interesting hybrid compounds were recently identified, starting from which, in this paper, a series of analogs were designed and synthesized. In particular, a thorough exploration of the cycloheptathiophene-3-carboxamide moiety led to acquire important SAR insight and identify new active compounds showing both the ability to inhibit PA-PB1 interaction and viral replication in the micromolar range and at non-toxic concentrations For few compounds, the ability to efficiently inhibit PA-PB1 subunits interaction did not translate into anti-Flu activity. Chem./phys. properties were investigated for a couple of compounds suggesting that the low solubility of compound I, due to a strong crystal lattice, may have impaired its antiviral activity. Finally, computational studies performed on compound II, in which the Ph ring suitably replaced the cycloheptathiophene, suggested that, in addition to hydrophobic interactions, H-bonds enhanced its binding within the PAC cavity. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Application of 683-57-8)
2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Application of 683-57-8
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