Nielsen, Daniel S. published the artcileHigh Cell Permeability Does Not Predict Oral Bioavailability for Analogues of Cyclic Heptapeptide Sanguinamide A*, Category: ethers-buliding-blocks, the publication is Australian Journal of Chemistry (2020), 73(4), 344-351, database is CAplus.
The cyclic heptapeptide derivative, sanguinamide A, is a model scaffold for studying how component amino acids, heterocycles, and N-methylation influence membrane permeability and oral bioavailability. Membrane permeable sanguinamide A analogs have been reported, but there is limited data on their pharmacokinetic properties in vivo. Here we report pharmacokinetic properties for highly cell and membrane permeable sanguinamide A analogs in rats and find that there is no correlation between reported permeability in vitro and oral bioavailability in vivo. We show that N-methylation of sanguinamide A analogs gives compounds with greater flexibility, greater susceptibility to degradation by rat liver microsomes, and lower oral bioavailability in rats.
Australian Journal of 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