CAS: 147123-47-5; 3-Aminothiophene-2-Carboxamide

相似化合物

56489-05-5 1378876-49-3 886497-80-9

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📜3-氨基-2-噻吩甲酰肼置于ni-Raney体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 4.0H,以20%的收率获得3-氨基噻吩-2-甲酰胺
参考文献: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
标题: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
摘要:Influenza Viruses (Flu) Are Responsible For Seasonal Epidemics Causing High Rates Of Morbidity,Which Can Dramatically Increase During Severe Pandemic Outbreaks. Antiviral Drugs Are An Indispensable Weapon To Treat Infected People And Reduce The Impact On Human Health,Nevertheless Anti-Flu Armamentarium Still Remains Inadequate. In Search For New Anti-Flu Drugs,Our Group Has 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 Analogues 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. Chemical/physical Properties Were Investigated For A Couple Of Compounds Suggesting That The Low Solubility Of Compound 14,Due To A Strong Crystal Lattice,May Have Impaired Its Antiviral Activity. Finally,Computational Studies Performed On Compound 23,In Which The Phenyl Ring Suitably Replaced The Cycloheptathiophene,Suggested That,In Addition To Hydrophobic Interactions,H-Bonds Enhanced Its Binding Within The Pac Cavity.
Doi:10.1016/j.Ejmech.2020.112944

专利信息

专利号:CN-108658999-B
优先权日:2018-04-24
标 题 :Synthesis method of 2-phenyl heterocyclic [2,3-d ] pyrimidine-4 (3H) -ketone compound