40871-01-0Relevant articles and documents
Iodine-alumina catalyzed Aza- michael addition under solvent free conditions
Saikia, Monmi,Kakati, Dwipen,Joseph, Maria Stalin,Sarma, Jadab Chandra
experimental part, p. 654 - 658 (2010/06/15)
An efficient aza-Michael addition of amines to a variety of activated olefins was carried out under solvent free conditions using iodine-alumina as a catalyst at room temperature or under microwave irradiation (in case of solid) in high yield. 2009 Bentham Science Publishers Ltd.
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.
Design and synthesis of potent and selective inhibitors of integrin VLA-4
Wattanasin, Sompong,Weidmann, Beat,Roche, Didier,Myers, Stewart,Xing, Amy,Guo, Qin,Sabio, Michael,Von Matt, Peter,Hugo, Ronald,Maida, Susan,Lake, Philip,Weetall, Marla
, p. 2955 - 2958 (2007/10/03)
The synthesis and identification of a novel series of inhibitors of integrin VLA-4 are described. Their in vitro activity and selectivity against closely related integrins are also presented.