Discovery of Neuritogenic Compound Classes Inspired by Natural Products

Neuritogenic Surfaces using Natural Product Analogs

“…By truncating natural product lead structures, several groups have identifi ed functionally optimized and structurally simplifi ed compounds. [ 22,26,27 ] However, in all these reports, experiments were carried out in solution, and, to the best of our knowledge, no study described the use of neuritogenic small molecules We chose to screen a range of different fi nal concentrations from 10 × 10 −9 to 10 × 10 −3 M , using the same experimental setup as described above. As can be seen in Figure 3 , surfaces generated from coating solution concentrations ranging from 1 × 10 −3 to 100 × 10 −9 M signifi cantly induced neurite outgrowth.…”

Synthesis of Neurotrophic Seco-prezizaane Sesquiterpenes (1R,10S)-2-Oxo-3,4-dehydroneomajucin, (2S)-Hydroxy-3,4-dehydroneomajucin, and (−)-Jiadifenin

“…1 While proteins that serve in this regard (neurotrophins) have been investigated as potential therapeutic agents, they suffer from a variety of suboptimal characteristics that negatively impact their potential utility in the clinic ( i.e. low serum stability, poor oral bioavailability, and inefficient penetration into the central nervous system).…”

“…low serum stability, poor oral bioavailability, and inefficient penetration into the central nervous system). 1a, 2 As such, there has been growing interest in identifying small molecule neurotrophic agents that have a more favorable pharmacokinetic profile. 3 While early investigations of the seeds of the Japanese star anise ( Illicium anisatum, L. ) delivered anisatin, 4 a neurotoxic noncompetitive GABA antagonist, 5 more recent studies of Illicium terrestrial plants (evergreen shrubs/trees) have delivered a collection of complex carbocyclic natural products that have been shown to possess potent neurotrophic properties (Figure 1).…”

Silver(I)‐Catalyzed Enantioselective [3+2]‐Cycloaddition Reaction of α‐Silylimines: A Facile Route to Quaternary‐Carbon‐Rich Scaffolds

“…Recently,w eh ad successfully explored amino-acid-derived chiral alkyldiphenylphosphines in asymmetric annulation reactions. [15] Amongt he two aminophosphines (3d-e)t ested, only the l-threonine derived one (3e)a fforded am oderate yield and improved enantioselectivity for the major syn-isomer of adduct 4a (entries 4-5). A chiral diamine-based phosphine ligand 3f also failed to provide the desired result (entry 6).…”