CAS: 865854-05-3; 4-Benzyl-2-(Naphthalen-1-yl)-1,2,4-Thiadiazolidine-3,5-Dione

上下游产品

Benzyl isothi°Cyanate 1-Naphthyl is°Cyanate

📜在 Air体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.5H,反应生成 4-苄基-2-(萘-1-基)-[1,2,4]噻二唑烷-3,5-二酮
参考文献:Tideglusib And Its Analogues As Inhibitors Of Staphylococcus Aureus Srta
标题:Tideglusib And Its Analogues As Inhibitors Of Staphylococcus Aureus Srta
摘要:Sortase A (Srta) Anchors Surface Proteins To The Cell Wall Envelope,And It Has Attracted Increasing Interesting As A Potential Antivirulence Target. Several Small-Molecule Inhibitors For Srta Have Been Developed,But Target Validation Remains Largely Underexplored. Herein,We Report A New Class Of Srta Inhibitors That Supports Antivirulence Therapy Through Small-Molecule Targeting Of Srta. Tideglusib (Td),A Drug Candidate For Myotonic Dystrophy,Was Outstanding In High-Throughput Screening. A Concise Synthetic Route Quickly Provided Td Analogues,And The Structure-Activity Relationships For Srta Inhibition Have Been Established From Those Analogues. Several Compounds Largely Retained The In Vitro Potency And Exhibited A Better Solubility Than Td. Additionally,Td Attenuated Virulence-Related Phenotypes In Vitro And Protected Mice Against Lethal S. Aureus Usa300 Bacteremia. Our Study Indicates That Td And Its Analogues Could Be New Candidates As Srta Inhibitors With Potential In The Development Of New Antivirulence Agents.
DOI:10.1021/acs.Jmedchem.0C00803