(S)-Glutamic acid (Glu), which is the main excitatory neurotransmitter in the central nervous
system (CNS), and other excitatory amino acids (EAAs) operate through four different classes …

The molecular biological revolution and the mapping of the human genome continue to
provide new challenges and opportunities for drug research and design. Future medicinal …

A rapid synthesis of aryl azides from the corresponding aryl halides catalyzed by CuI/diamine
is described. Sodium ascorbate was found to have a positive effect on stabilization of the …

Ionotropic glutamate receptors (iGluRs) constitute a family of ligand-gated ion channels that
are essential for mediating fast synaptic transmission in the central nervous system. These …

Building on the success of the previous editions, Textbook of Drug Design and Discovery
has been thoroughly revised and updated to provide a complete source of information on all …

Dimeric positive allosteric modulators of ionotropic glutamate receptors were designed,
synthesized, and characterized pharmacologically in electrophysiological experiments. The …

More than 50 structures have been reported on the ligand-binding core of the ionotropic
glutamate receptor iGluR2 that belongs to the 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)…

A number of 1-hydroxyazole derivatives were synthesized as bioisosteres of (S)-glutamic
acid (Glu) and as analogues of the AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-…

The four stereoisomers of 5-(2-amino-2-carboxyethyl)-4,5-dihydroisoxazole-3-carboxylic
acid(+)-4, (−)-4, (+)-5, and (−)-5 were prepared by stereoselective synthesis of two pairs of …

The design and synthesis of conformationally restricted analogues of α-amino acids is an
often used strategy in medicinal chemistry research. Here we present the rational design, …