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Updated: Jan 18, 2026

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides
Prakash Chaudhari1, Ashley Bunnell1, Manivannan Yegambaram1
1Department of Cellular Biology & Pharmacology, Herbert Wertheim College of Medicine, Florida International University, Center for Translational Science, Port Saint Lucie, FL 34987, USA.
None:
Diaza-peptidomimetics are constrained compounds that mimic the biological efficacy of peptides while offering increased stability. We have previously reported the synthesis of bis-cyclic guanidine heterocyclic peptidomimetics as opioid ligands with mixed μ-, κ- and δ-opioid receptor interactions and their potential activity as novel analgesics. Using the same approach, we report here the synthesis of sulfonated and piperazine-tethered bis-cyclic guanidines and their in vitro screening results from radioligand competition binding assays at the μ- (MOR), δ- (DOR), and κ- (KOR) opioid receptors.
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