Apis group Amino acids, Peptidomimetics, peptides, protein InteractionS group

Non-natural 3‑Arylmorpholino-β-amino Acid as a PPII Helix Inducer

A new non-natural β-amino acid, named 3-Ar-β-Morph, was designed and synthesized via a regio- and diastereoselective Pdcatalyzed C(sp3)H-arylation of the corresponding 2S,6S-(6-methoxymorpholin-2-yl)carboxylic acid, readily available from glucose. According to the computational prevision and confirmed...

The selective disruption of presynaptic JNK2/STX1a interaction reduces NMDA receptor-dependent glutamate release

The neuronal loss caused by excessive glutamate release, or ‘excitotoxicity’, leads to several pathological conditions, including cerebral ischemia, epilepsy, and neurodegenerative diseases. Over-stimulation of presynaptic N-methyl-D-aspartate (NMDA) receptors is known to trigger and support...

Stereoselective Synthesis of α,α′-Dihydroxy-beta, beta′-diaryl-beta-amino Acids by Mannich-Like Condensation of Hydroarylamides

Dual α,α′-Dihydroxy-beta,beta’-beta-amino acids are highly interesting tools for several industrial applications. Nevertheless, only few derivatives are reported in the literature and knowledge concerning the substitution pattern as well as their enantioselective syntheses are lacking....

On‑resin multicomponent 1,3‑dipolar cycloaddition of cyclopentanone–proline enamines and sulfonylazides as an efficient tool for the synthesis of amidino depsipeptide mimics

Depsipeptides are biologically active peptide derivatives that possess a high therapeutic interest. The development of depsipeptide mimics characterized by a chemical diversity could lead to compounds with enhanced features and activity. In this work,...