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Updated: Jul 9, 2026
Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
Protected aminooxyprolines for expedited library synthesis: application to Tsg101-directed proline-oxime containing
Fa Liu1, Andrew G Stephen, Robert J Fisher
1Laboratory of Medicinal Chemistry, CCR, NCI-Frederick, NIH, Building 376 Boyles Street, Frederick, MD 21702, USA.
Abstract:
The stereoselective synthesis of aminooxy-containing proline analogues bearing Fmoc/Boc or Fmoc/Mtt protection that renders them suitable for incorporation into peptides using Fmoc protocols is reported. Acid-catalyzed unmasking at the completion of peptide synthesis yields free aminooxy-functionalities for oxime formation through reaction with libraries of aldehydes. This allows post solid-phase diversification strategies that may facilitate structure-activity relationship studies.
