Ontology highlight
ABSTRACT:
SUBMITTER: White TR
PROVIDER: S-EPMC3210067 | biostudies-literature | 2011 Sep
REPOSITORIES: biostudies-literature
Nature chemical biology 20110925 11
Backbone N-methylation is common among peptide natural products and has a substantial impact on both the physical properties and the conformational states of cyclic peptides. However, the specific impact of N-methylation on passive membrane diffusion in cyclic peptides has not been investigated systematically. Here we report a method for the selective, on-resin N-methylation of cyclic peptides to generate compounds with drug-like membrane permeability and oral bioavailability. The selectivity an ...[more]