Pismataro, Maria Chiara published the artcile1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors, HPLC of Formula: 1455-77-2, the main research area is triazolopyrimidine preparation antiviral influenza polymerase PA PB1 interaction disruptor; 1,2,4-triazolo[1,5-a]pyrimidines; Antiviral agents; Influenza polymerase; Influenza virus; PA-PB1 interaction; Protein-protein interaction; SARS-CoV-2.
In the search for new anti-influenza virus (IV) compounds, the 1,2,4-triazolo[1,5-a]pyrimidine (TZP) was identified as a very suitable scaffold to obtain compounds able to disrupt IV RNA-dependent RNA polymerase (RdRP) PA-PB1 subunits heterodimerization. To this aim, four facile and efficient one-step procedures for the synthesis of 5-phenyl-, 6-phenyl- and 7-phenyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidines, and 2-amino-5-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ol has been developed. Two analogs having the Et carboxylate moiety at the C-2 position of the TZP were also prepared in good yields. Then, the scaffolds herein synthesized and two previous scaffolds were functionalized and evaluated for their anti-IAV activity, leading to the identification of compound 2-(5-Methyl-7-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)-4H-benzo[d][1,3]oxazin-4-one that showed both anti-PA-PB1 (IC50 = 19.5μM) and anti-IAV activity (EC50 = 16μM) at non-toxic concentrations, thus resulting among the most active TZP derivatives reported to date by us. A selection of the synthesized compounds, along with a set of inhouse available analogs, was also tested against SARS-CoV-2. The most promising compound N-(2-Fluorophenyl)-7-methyl-5-phenyl-[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxamide from this series displayed an EC50 value of 34.47μM, highlighting the potential of the TPZ scaffold in the search for anti-CoV agents.
European Journal of Medicinal Chemistry published new progress about Antiviral agents. 1455-77-2 belongs to class isoquinoline, name is 3,5-Diamino-1,2,4-triazole, and the molecular formula is C2H5N5, HPLC of Formula: 1455-77-2.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem