01423nas a2200181   4500008004100000245012200041210006900163260000800232300001400240490000600254520071400260100003500974700002401009700002501033700002601058700002801084856012901112       2017                        eng d00aRigid peptide scaffold-incorporated structural analogs of the potent antidepressant peptide drug rapastinel (GLYX-13)0 aRigid peptide scaffoldincorporated structural analogs of the pot  cAPR  a3594-35960 v23 a<p>Rapastinel (GLYX-13) is a natural amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2)endowed with strong antidepressant property. Rapastinel shows considerable promise for treating drug-resistant major depressive disorder (MDD), and is under clinical phase III development. Herein, we report the synthesis of a novel class of analogues of the potent antidepressant peptide drug rapastinel featuring rigid dipeptide scaffolds comprising proline (L/D) and amino thiophene carboxylates (Atc). Amino thiophene carboxylate is a conformationally constrained aromatic beta-amino acid, known to rigidify peptide backbones thereby limiting the conformational flexibility of peptides and improving proteolytic stability.</p>1 aNadimpally, Krishna, Chaitanya1 aChakrapani, Aswathi1 aPrabhu, Priyanka, J.1 aMadica, Krishnaprasad1 aSanjayan, Gangadhar, J.  uhttps://library.ncl.res.in/content/rigid-peptide-scaffold-incorporated-structural-analogs-potent-antidepressant-peptide-drug