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On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds
- White, Tina R;
- Renzelman, Chad M;
- Rand, Arthur C;
- Rezai, Taha;
- McEwen, Cayla M;
- Gelev, Vladimir M;
- Turner, Rushia A;
- Linington, Roger G;
- Leung, Siegfried SF;
- Kalgutkar, Amit S;
- Bauman, Jonathan N;
- Zhang, Yizhong;
- Liras, Spiros;
- Price, David A;
- Mathiowetz, Alan M;
- Jacobson, Matthew P;
- Lokey, R Scott
Published Web Location
https://doi.org/10.1038/nchembio.664Abstract
A single trimethylated species is obtained in an on-resin N-methylation reaction of a cyclic hexapeptide. This regioselectivity is driven by conformation and the presence of intramolecular hydrogen bonds, and is correlated with membrane permeability of the peptides.
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