Rochon, Kristina’s team published research in ACS Chemical Neuroscience in 4 | CAS: 77128-73-5

ACS Chemical Neuroscience published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, Application of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid.

Rochon, Kristina published the artcilePreparation and Evaluation at the Delta Opioid Receptor of a Series of Linear Leu-Enkephalin Analogues Obtained by Systematic Replacement of the Amides, Application of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, the publication is ACS Chemical Neuroscience (2013), 4(8), 1204-1216, database is CAplus and MEDLINE.

Leu-enkephalin analogs, in which the amide bonds were sequentially and systematically replaced either by ester or N-Me amide bonds, were prepared using classical organic chem. as well as solid-phase peptide synthesis (SPPS). The peptidomimetics were characterized using competition binding, ERK1/2 phosphorylation, receptor internalization, and contractility assays to evaluate their pharmacol. profile over the delta opioid receptor (DOPr). The lipophilicity (LogD7.4) and plasma stability of the active analogs were also measured. The results here revealed that the last amide bond can be successfully replaced by either an ester or an N-Me amide bond without significantly decreasing the biol. activity of the corresponding analogs when compared to Leu-enkephalin. The peptidomimetics with an N-Me amide function between residues Phe and Leu were found to be more lipophilic and more stable than Leu-enkephalin. Findings from the present study further revealed that the hydrogen-bond donor properties of the fourth amide of Leu-enkephalin are not important for its biol. activity on DOPr. In addition, the results showed that the systematic replacement of amide bonds by isosteric functions represents an efficient way to design and synthesize novel peptide analogs with enhanced stability. In conclusion, the authors suggest that such a strategy can also be useful to study the biol. roles of amide bonds.

ACS Chemical Neuroscience published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, Application of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem