Pismataro, MC; Felicetti, T; Bertagnin, C; Nizi, MG; Bonomini, A; Barreca, ML; Cecchetti, V; Jochmans, D; De Jonghe, S; Neyts, J; Loregian, A; Tabarrini, O; Massari, S in [Pismataro, Maria Chiara; Felicetti, Tommaso; Nizi, Maria Giulia; Barreca, Maria Letizia; Cecchetti, Violetta; Tabarrini, Oriana; Massari, Serena] Univ Perugia, Dept Pharmaceut Sci, Via Del Liceo 1, I-06123 Perugia, Italy; [Bertagnin, Chiara; Bonomini, Anna; Loregian, Arianna] Univ Padua, Dept Mol Med, Via Gabelli 63, I-35121 Padua, Italy; [Jochmans, Dirk; De Jonghe, Steven; Neyts, Johan] Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Rega Inst Med Res, Lab Virol & Chemotherapy, Herestr 49,Box 1043, B-3000 Leuven, Belgium published 1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors in 2021, Cited 46. Category: thiomorpholine. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.
In the search for new anti-influenza virus (IV) compounds, we have identified the 1,2,4-triazolo[1,5-a] pyrimidine (TZP) as a very suitable scaffold to obtain compounds able to disrupt IV RNA-dependent RNA polymerase (RdRP) PA-PB1 subunits heterodimerization. In this work, in order to acquire further SAR insights for this class of compounds and identify more potent derivatives, we designed and synthesized additional series of analogues to investigate the role of the substituents around the TZP core. To this aim, we developed 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. Two analogues having the ethyl 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 22 that showed both anti-PA-PB1 (IC50 = 19.5 mM) and anti-IAV activity (EC50 = 16 mM) 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 in-house available analogues, was also tested against SARS-CoV-2. The most promising compound 49 from this series displayed an EC50 value of 34.47 mM, high-lighting the potential of the TPZ scaffold in the search for anti-CoV agents. (C) 2021 Elsevier Masson SAS. All rights reserved.
Welcome to talk about 88-68-6, If you have any questions, you can contact Pismataro, MC; Felicetti, T; Bertagnin, C; Nizi, MG; Bonomini, A; Barreca, ML; Cecchetti, V; Jochmans, D; De Jonghe, S; Neyts, J; Loregian, A; Tabarrini, O; Massari, S or send Email.. Category: thiomorpholine
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem