Issue 43, 2021

Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides

Abstract

Here, we investigated the effect of CH3 to CF3 substitution on the membrane permeability of peptides. We synthesized a series of peptides with CF3 groups and corresponding nonfluorinated peptides and measured the membrane permeability of the peptides. As a result, we demonstrated that CH3 to CF3 substitution is useful for increasing the membrane permeability of di-/tri-peptides.

Graphical abstract: Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides

Supplementary files

Article information

Article type
Communication
Submitted
09 Aug. 2021
Accepted
13 Okt. 2021
First published
13 Okt. 2021

Org. Biomol. Chem., 2021,19, 9386-9389

Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides

T. Ono, K. Aikawa, T. Okazoe, J. Morimoto and S. Sando, Org. Biomol. Chem., 2021, 19, 9386 DOI: 10.1039/D1OB01565F

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