Barraza, Scott J.; Sindac, Janice A.; Dobry, Craig J.; Delekta, Philip C.; Lee, Pil H.; Miller, David J.; Larsen, Scott D. published the artcile< Synthesis and biological activity of conformationally restricted indole-based inhibitors of neurotropic alphavirus replication: Generation of a three-dimensional pharmacophore>, Application In Synthesis of 3731-53-1, the main research area is indole preparation neurotropic alphavirus replication inhibitor; Antiviral; Conformationally restricted; Neurotropic alphavirus; Pharmacophore; Western equine encephalitis virus.
Authors have previously reported the development of indole-based CNS-active antivirals for the treatment of neurotropic alphavirus infection, but further optimization is impeded by a lack of knowledge of the mol. target and binding site. Herein authors describe the design, synthesis and evaluation of a series of conformationally restricted analogs with the dual objectives of improving potency/selectivity and identifying the most bioactive conformation. Although this campaign was only modestly successful at improving potency, the sharply defined SAR of the rigid analogs enabled the definition of a three-dimensional pharmacophore, which authors believe will be of value in further analog design and virtual screening for alternative antiviral leads.
Bioorganic & Medicinal Chemistry Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Application In Synthesis of 3731-53-1.