Lefever, Mark’s team published research in Journal of Medicinal Chemistry in 58 | CAS: 77128-73-5

Lefever, Mark published the artcileStructural Requirements for CNS Active Opioid Glycopeptides, Category: ethers-buliding-blocks, the publication is Journal of Medicinal Chemistry (2015), 58(15), 5728-5741, database is CAplus and MEDLINE.

Glycopeptides related to β-endorphin penetrate the blood-brain barrier (BBB) of mice to produce antinociception. Two series of glycopeptides were assessed for opioid receptor binding affinity. Attempts to alter the mu-selectivity of [D-Ala²,N-MePhe⁴,Gly-ol⁵]enkephalin (DAMGO)-related glycopeptides by altering the charged residues of the amphipathic helical address were unsuccessful. A series of pan-agonists was evaluated for antinociceptive activity (55 °C tail flick) in mice. A flexible linker was required to maintain antinociceptive activity. CD in H₂O, trifluoroethanol (TFE), and SDS micelles confirmed the importance of the amphipathic helixes (11s â†?11sG â†?11) for antinociception. The glycosylated analogs showed only nascent helixes and random coil conformations in H₂O. Chem. shift indexes (CSI) and nuclear Overhauser effects (NOE) with 600 MHz NMR and CD confirmed helical structures in micelles, which were rationalized by mol. dynamics calculations Antinociceptive studies with mice confirm that these glycosylated endorphin analogs are potential drug candidates that penetrate the BBB to produce potent central effects.

Journal of Medicinal Chemistry 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, Category: ethers-buliding-blocks.

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