Issue 47, 2021

A comprehensive study on the effect of backbone stereochemistry of a cyclic hexapeptide on membrane permeability and microsomal stability

Abstract

Backbone stereochemistry of cyclic peptides has been reported to have a great influence on microsomal stability and membrane permeability, two important factors that determine oral bioavailability. Here, we comprehensively investigated the correlation between the backbone stereochemistry of cyclic hexapeptide stereoisomers and their stability in liver microsomes, as well as passive membrane permeability.

Graphical abstract: A comprehensive study on the effect of backbone stereochemistry of a cyclic hexapeptide on membrane permeability and microsomal stability

Supplementary files

Article information

Article type
Communication
Submitted
25 oct. 2021
Accepted
21 nov. 2021
First published
22 nov. 2021

Org. Biomol. Chem., 2021,19, 10326-10331

Author version available

A comprehensive study on the effect of backbone stereochemistry of a cyclic hexapeptide on membrane permeability and microsomal stability

Y. Hosono, J. Morimoto and S. Sando, Org. Biomol. Chem., 2021, 19, 10326 DOI: 10.1039/D1OB02090K

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