Hydrazinverbindungen als Heterobestandteile in Peptiden, IX. Synthese des Eledoisin‐(4‐11)‐Octapeptides Lys‐Asp(NH
2
)‐Ala‐Phe‐Ile‐Gly‐Leu‐Met‐NH
2
und seines Heterologen mit Hydrazinoessigsäure statt Glycin
摘要:
AbstractDie Verknüpfung zweier Tetrapeptide nach der Azid‐Methode liefert das Eledoisin‐(4–11)‐Octapeptid ·2 TFA (6). Nach Kondensation (Phosphorazo‐Methode) von Z‐ bzw. Boc‐Ile‐NHGly(Nα‐Boc)‐OH mit Leu‐Met‐NH2erlaubt die gleiche Synthese mit dem Nα‐ungeschützten Heterotetrapeptid10, aus dem Reaktionsgemisch das [5‐Asparagin, 9‐Hydrazino‐essigsäure]Eledoisin‐(4‐11)‐Octapeptid‐Acetat (11) zu isolieren.
Hydrazino and N-Amino peptides. Chemical and structural aspects
作者:Alain Lecoq、Michel Marraud、André Aubry
DOI:10.1016/0040-4039(91)85080-o
日期:1991.6
The regioselective acylation of the nitrogens in hydrazino acetic acid has been studied to obtain the hydrazide and N-amino amide peptidomimetic groups Their conformational influence on the β-turn structure has also been considered.
The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
Glycogen synthase (GS) catalyzes the transfer of glucose residues from UDP-glucose to a glycogen polymer chain, a critical step for glucose storage. Patients with type 2 diabetes normally exhibit low glycogen levels and decreased muscle glucose uptake is the major defect in whole body glucose disposal. Therefore, activating GS may provide a potential approach for the treatment of type 2 diabetes. In order to identify non-carboxylic acids GS activators, we designed and synthesized a series of 2-N-alkyl- and 2-N-aryl-indazolone derivatives and studied their activity in activating human GS. (C) 2013 Elsevier Ltd. All rights reserved.
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