118447-04-4Relevant academic research and scientific papers
Proline-based reduced dipeptides as recyclable and highly enantioselective organocatalysts for asymmetric Michael addition
Cao, Xiaohui,Wang, Ge,Zhang, Richeng,Wei, Yingying,Wang, Wei,Sun, Huichao,Chen, Ligong
, p. 6487 - 6490 (2011/11/05)
A series of novel proline-based reduced dipeptides was developed and evaluated for a direct Michael addition of ketones and aldehydes to nitroalkenes. Excellent yields (up to 95%), diastereoselectivities (up to 98% dr) and enantioselectivities (up to 98%
New Modified Heterocyclic Phenylalanine Derivatives. Incorporation into Potent Inhibitors of Human Renin
Ocain, Timothy D.,Deininger, David D.,Russo, Ralph,Senko, Nancie A.,Katz, Alan,et al.
, p. 823 - 832 (2007/10/02)
Modified heterocyclic phenylalanine analogues designed as replacements for the P3-P4 region were synthesized and incorporated into renin inhibitors.These inhibitors were found to have significant activity versus human recombinant renin, as well as in vivo activity.The compounds proved to be very resistant to chymotrypsin degradation, as exemplified by compound 8, which remained greater than 60percent intact after a 24-h exposure to chymotrypsin.In contrast, the Boc-Phe analogue was nearly completely degraded after 1 h.Compound 6 proved to be the most potent renin inhibitor with an IC50=8.9 nM.These stable cyclized phenylalanines should prove to be generally useful as a substitute for Boc-Phe in protease inhibitors.
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The synthesis of bradykinin analogues is described in which the Gly4-Phe5, Phe5-Ser6 or the Pro7-Phe8 peptide bond has been replaced by a trans carbon-carbon double bond or by a "reduced" peptide bond.Some of the analogues display high potency and prolonged activity in the rat blood pressure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.
