In 2018,Pomplun, Sebastian; Sippel, Claudia; Haehle, Andreas; Tay, Donald; Shima, Kensuke; Klages, Alina; Uenal, Can Murat; Riess, Benedikt; Toh, Hui Ting; Hansen, Guido; Yoon, Ho Sup; Bracher, Andreas; Preiser, Peter; Rupp, Jan; Steinert, Michael; Hausch, Felix published 《Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins》.Journal of Medicinal Chemistry published the findings.Name: 2-(Bromomethyl)pyridine hydrobromide The information in the text is summarized as follows:
FK506-binding proteins (FKBPs) are evolutionarily conserved proteins that display peptidyl-prolyl isomerase activities and act as coreceptors for immunosuppressants. Microbial macrophage-infectivity-potentiator (Mip)-type FKBPs can enhance infectivity. However, developing druglike ligands for FKBPs or Mips has proven difficult, and many FKBPs and Mips still lack biol. useful ligands. To explore the scope and potential of C5-substituted [4.3.1]-aza-bicyclic sulfonamides as a broadly applicable class of FKBP inhibitors, we developed a new synthesis method for the bicyclic core scaffold and used it to prepare an FKBP- and Mip-focused library. This allowed us to perform a systematic structure-activity-relationship anal. across key human FKBPs and microbial Mips, yielding highly improved inhibitors for all the FKBPs studied. A cocrystal structure confirmed the mol.-binding mode of the core structure and explained the affinity gained as a result of the preferred substituents. The best FKBP and Mip ligands showed promising antimalarial, antileginonellal, and antichlamydial properties in cellular models of infectivity, suggesting that substituted [4.3.1]-aza-bicyclic sulfonamides could be a novel class of anti-infectives. In addition to this study using 2-(Bromomethyl)pyridine hydrobromide, there are many other studies that have used 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Name: 2-(Bromomethyl)pyridine hydrobromide) was used in this study.
2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Name: 2-(Bromomethyl)pyridine hydrobromide