543700-16-9Relevant academic research and scientific papers
TiCl4-promoted addition of nucleophiles to open chain α-amidoalkylphenyl sulfones
Petrini, Marino,Torregiani, Elisabetta
, p. 5999 - 6003 (2007/10/03)
Linear α-amidoalkylphenyl sulfones are converted into the corresponding N-acyliminium ions by treatment with TiCl4 at low temperature and then made to react with different nucleophiles such as allyltrimethylsilane, silyl ketene acetal, anisole
N-, α-, and β-substituted 3-aminopropionic acids: Design, syntheses and antiseizure activities
Tan,Wainman,Weaver
, p. 113 - 121 (2007/10/03)
A treatment for epilepsy is proposed based on analogues of 3-aminopropionic acid (β-alanine), a putative neurotransmitter in the central nervous system (CNS). A model three point pharmacophore was proposed based on modelling data obtained from the study of antagonists for both the glial γ-aminobutyric acid (GABA)-uptake site and the glycine co-agonist site of N-methyl-D-aspartate (NMDA) receptor. Three series of 3-aminopropionic acids containing, N-, α-, and β-substituents, were designed and synthesized to probe the position and the size of a lipophilic binding pocket within the proposed pharmacophore. These analogues were tested in vivo for both their antiseizure activities and their neurologic toxicities. Among the fourteen novel 3-aminopropionic acids synthesized, eight were found to have promising antiseizure activity. This study shows that substitution on the N-terminus confers the greatest antiseizure activity, particularly against pilocarpine-induced seizures.
