79839-29-5Relevant academic research and scientific papers
Synthesis and characterization of bradykinin B2 receptor agonists containing constrained dipeptide mimics
Amblard, Muriel,Daffix, Isabelle,Bergé, Gilbert,Calmès, Monique,Dodey, Pierre,Pruneau, Didier,Paquet, Jean-Luc,Luccarini, Jean-Michel,Bélichard, Pierre,Martinez, Jean
, p. 4193 - 4201 (2007/10/03)
We have previously shown that substitution of the D-Tic-Oic dipeptide by a (3S)-[amino]-5-(carbonylmethyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one (D-BT) moiety in the bradykinin B2 receptor antagonist HOE 140 resulted in a full potent and sel
Protected Lactam-Bridged Dipeptides for Use as Conformational Constraints in Peptides
Freidinger, Roger M.,Perlow, Debra Schwenk,Veber, Daniel F.
, p. 104 - 109 (2007/10/02)
General methods have been devised for the synthesis of lactam-constrained dipeptide analogues having five-, six-, and seven-membered rings.Three different paths from protected chiral α-amino acids to lactams involving intramolecular alkylation, intramolecular acylation, and insertion of a one carbon unit by condensation with formaldehyde have been utilized.The first two methods produce chiral products stereospecifically, but considerable racemization occurs in the third route which leads to a 4-oxo-5-amino-1,3-thiazine (13).The products are prepared in good yield and have protecting groups making them suitable for incorporation into higher peptides by methods commonly used.
