124339-42-0Relevant academic research and scientific papers
E-olefin dipeptide isostere incorporation into a polypeptide backbone enables hydrogen bond perturbation: Probing the requirements for Alzheimer's amyloidogenesis
Fu, Yanwen,Bieschke, Jan,Kelly, Jeffery W.
, p. 15366 - 15367 (2005)
Herein, we report a stereospecific E-olefin dipeptide isostere synthesis that can be used to make gram quantities of the Phe-Phe isostere desired for eliminating a specific backbone H-bond donor and acceptor in the Alzheimer's disease related Aβ peptide.
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BRADYKININ ANALOGUES WITH Ψ(E,CH=CH) AND Ψ(CH2-NH) ISOSTERIC PEPTIDE BOND REPLACEMENTS
Scarso, A.,Degelaen, J.,Viville, R.,Cock, E. De,Marsenille, M. Van,et al.
, p. 381 - 399 (2007/10/02)
The synthesis of bradykinin analogues is described in which the Gly4-Phe5, Phe5-Ser6 or the Pro7-Phe8 peptide bond has been replaced by a trans carbon-carbon double bond or by a "reduced" peptide bond.Some of the analogues display high potency and prolonged activity in the rat blood pressure test, indicating increased metabolic stability.A clear selectivity is obtained towards the myotropic effect in the guinea pig ileum.
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites
Kaltenbronn,Hudspeth,Lunney,Michniewicz,Nicolaides,Repine,Roark,Stier,Tinney,Woo,Essenburg
, p. 838 - 845 (2007/10/02)
Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these compounds are discussed. The two most potent compounds, 47 and 48, contai
